Hydrocortisone

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Identification

Summary

Hydrocortisone is a glucocorticoid used to treat corticosteroid-responsive dermatoses, endocrine disorders, immune conditions, and allergic disorders.

Brand Names

Ala-cort, Ala-scalp, Alcortin, Alkindi, Anusol HC, Aquanil HC, Casporyn HC, Cipro, Cipro HC, Colocort, Cortaid, Cortane-B, Cortef, Cortenema, Cortisporin, Cortizone-10, Dermacort, Dermarest Eczema, Dermazene, Home Papkit, Hydroskin, Monistat Itch Relief, Preparation H Hydrocortisone, Procto-med, Procto-pak, Proctocort, Proctol, Proctosol, Proctozone HC, Scalpicin Itch Relief, Texacort, Vanoxide-HC, Xerese

Generic Name

Hydrocortisone

DrugBank Accession Number

DB00741

Background

Hydrocortisone, or cortisol, is a glucocorticoid secreted by the adrenal cortex.⁷ Hydrocortisone is used to treat immune, inflammatory, and neoplastic conditions.^{14,15,16,17,18,19} It was discovered in the 1930s by Edward Kendall and named Compound F, or 17-hydroxycorticosterone.⁹

Hydrocortisone was granted FDA approval on 5 August 1952.²⁰

Type

Small Molecule

Groups

Approved, Vet approved

Structure

Similar Structures

Weight: Average: 362.4599
Monoisotopic: 362.20932407
Chemical Formula: C₂₁H₃₀O₅

Synonyms

(11β)-11,17,21-trihydroxypregn-4-ene-3,20-dione
11beta-hydrocortisone
11beta,17alpha,21-Trihydroxy-4-pregnene-3,20-dione
11β-hydrocortisone
17-Hydroxycorticosterone
4-pregnen-11β,17α,21-triol-3,20-dione
Cortisol
Hidrocortisona
Hydrocortisone
Hydrocortisonum
Kendall's compound F
Reichstein's substance M

External IDs

NSC-10483

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Pharmacology

Indication

Otic solutions are indicated for infections of the external auditory canal caused by susceptible organisms and with inflammation.^14,15 Hydrocortisone tablets are indicated for certain endocrine, rheumatic, collagen, allergic, ophthalmic, respiratory, hematologic, neoplastic, edematous, gastrointestinal, and other conditions.¹⁶ A hydrocortisone enema is indicated for ulcerative colitis,¹⁷ a topical ointment with antibiotics is indicated for corticosteroid responsive dermatoses with infections,¹⁸ and a topical cream with acyclovir is indicated to treat cold sores.¹⁹ Oral granules of hydrocortisone are used as a replacement therapy for Adrenocortical Insufficiency (AI) in children under 17 years of age.²¹

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Associated Conditions

Indication Type	Indication	Combined Product Details	Approval Level	Age Group	Dose Form
Treatment of	Acquired hemolytic anemia		••••••••••••	•••••	••••••
Management of	Acute gouty arthritis		••••••••••••		••••••
Symptomatic treatment of	Acute leukemia		••••••••••••	•••••••••	••••••
Used in combination to treat	Acute otitis externa	Combination Product in combination with: Ciprofloxacin (DB00537)	••••••••••••		•••••••• • •••••
Treatment of	Adrenal insufficiency		••••••••••••	••••••••••• •••••••••	•••••••

Associated Therapies

Palliatives Treatments

Contraindications & Blackbox Warnings

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Pharmacodynamics

Hydrocortisone binds to the glucocorticoid receptor leading to downstream effects such as inhibition of phospholipase A2, NF-kappa B, other inflammatory transcription factors, and the promotion of anti-inflammatory genes.¹⁰ Hydrocortisone has a wide therapeutic index⁸ and a moderate duration of action.^1,6 Patients should stop taking the medication if irritation or sensitization occurs.^{14,15,16,17,18,19}

Mechanism of action

The short term effects of corticosteroids are decreased vasodilation and permeability of capillaries, as well as decreased leukocyte migration to sites of inflammation.¹⁰ Corticosteroids binding to the glucocorticoid receptor mediates changes in gene expression that lead to multiple downstream effects over hours to days.¹⁰

Glucocorticoids inhibit neutrophil apoptosis and demargination; they inhibit phospholipase A2, which decreases the formation of arachidonic acid derivatives; they inhibit NF-Kappa B and other inflammatory transcription factors; they promote anti-inflammatory genes like interleukin-10.¹⁰

Lower doses of corticosteroids provide an anti-inflammatory effect, while higher doses are immunosuppressive.¹⁰ High doses of glucocorticoids for an extended period bind to the mineralocorticoid receptor, raising sodium levels and decreasing potassium levels.¹⁰

Target	Actions	Organism
AGlucocorticoid receptor	agonist	Humans
AAnnexin A1	agonist	Humans

Absorption

Oral hydrocortisone at a dose of 0.2-0.3mg/kg/day reached a mean C_max of 32.69nmol/L with a mean AUC of 90.63h*nmol/L¹ A 0.4-0.6mg/kg/day dose reached a mean C_max of 70.81nmol/L with a mean AUC of 199.11h*nmol/L.¹ However, the pharmacokinetics of hydrocortisone can vary by 10 times from patient to patient.¹

Topical hydrocortisone cream is 4-19% bioavailable³ with a T_max of 24h.²

Hydrocortisone retention enemas are have a bioavailability of 0.810 for slow absorbers and 0.502 in rapid absorbers.⁴ Slow absorbers take up hydrocortisone at a rate of 0.361±0.255/h while fast absorbers take up hydrocortisone at a rate of 1.05±0.255/h.⁴

A 20mg IV dose of hydrocortisone has an AUC of 1163±277ng*h/mL.⁶

Volume of distribution

Total hydrocortisone has a volume of distribution of 39.82L, while the free fraction has a volume of distribution of 474.38L.¹

Protein binding

Corticosteroids are generally bound to corticosteroid binding globulin¹¹ and serum albumin¹² in plasma. Hydrocortisone is 90.1% bound to proteins in plasma, with 56.2% bound to albumin.⁵

Metabolism

Hydrocortisone is metabolised to 6-beta hydrocortisol via CYP3A, 5-beta tetrahydrocortisol via 3-oxo-5-beta-steroid 4-dehydrogenase, 5-alpha tetrahydrocortisol via 3-oxo-5-alpha-steroid 4-dehydrogenase 2, cortisone via Corticosteroid 11-beta-dehydrogenase isozyme 1 and Corticosteroid 11-beta-dehydrogenase isozyme 2, and glucuronide products.¹³ Cortisone is further metabolized to tetrahydrocortisone and dihydrocortisol.¹³

Hover over products below to view reaction partners

Hydrocortisone

Route of elimination

Corticosteroids are eliminated predominantly in the urine.¹² However, data regarding the exact proportion is not readily available.⁷

Half-life

Total hydrocortisone via the oral route has a half life of 2.15h while the free fraction has a half life of 1.39h.¹ A 20mg IV dose of hydrocortisone has a terminal half life of 1.9±0.4h.⁶

Clearance

Total hydrocortisone by the oral route has a mean clearance of 12.85L/h, while the free fraction has a mean clearance of 235.78L/h.¹ A 20mg IV dose of hydrocortisone has a clearance of 18.2±4.2L/h.⁶

Adverse Effects

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Toxicity

Data regarding acute overdoses of glucocorticoids are rare.^{14,15,16,17,18,19} Chronic high doses of glucocorticoids can lead to the development of cataract, glaucoma, hypertension, water retention, hyperlipidemia, peptic ulcer, pancreatitis, myopathy, osteoporosis, mood changes, psychosis, dermal atrophy, allergy, acne, hypertrichosis, immune suppression, decreased resistance to infection, moon face, hyperglycemia, hypocalcemia, hypophosphatemia, metabolic acidosis, growth suppression, and secondary adrenal insufficiency.⁸ Overdose may be treated by adjusting the dose or stopping the corticosteroid as well as initiating symptomatic and supportive treatment.⁸

Pathways

Pathway	Category
Adrenal Hyperplasia Type 5 or Congenital Adrenal Hyperplasia Due to 17 alpha-Hydroxylase Deficiency	Disease
Corticosterone Methyl Oxidase I Deficiency (CMO I)	Disease
3-beta-Hydroxysteroid Dehydrogenase Deficiency	Disease
Corticotropin Activation of Cortisol Production	Signaling
Congenital Lipoid Adrenal Hyperplasia (CLAH) or Lipoid CAH	Disease
11-beta-Hydroxylase Deficiency (CYP11B1)	Disease
Apparent Mineralocorticoid Excess Syndrome	Disease
Steroidogenesis	Metabolic
Adrenal Hyperplasia Type 3 or Congenital Adrenal Hyperplasia Due to 21-Hydroxylase Deficiency	Disease
17-alpha-Hydroxylase Deficiency (CYP17)	Disease
21-Hydroxylase Deficiency (CYP21)	Disease
Corticosterone Methyl Oxidase II Deficiency (CMO II)	Disease

Pharmacogenomic Effects/ADRs

Not Available

Interactions

Drug Interactions

This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.

Drug	Interaction
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Abametapir	The serum concentration of Hydrocortisone can be increased when it is combined with Abametapir.
Abatacept	The metabolism of Hydrocortisone can be increased when combined with Abatacept.
Abemaciclib	The metabolism of Abemaciclib can be increased when combined with Hydrocortisone.
Acalabrutinib	The metabolism of Acalabrutinib can be increased when combined with Hydrocortisone.
Acarbose	The risk or severity of hyperglycemia can be increased when Hydrocortisone is combined with Acarbose.

Food Interactions

Avoid alcohol.

Products

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Product Images

International/Other Brands

Acticort / Aeroseb HC / Ala-Scalp / Algicirtis / Beta-HC / Cetacort / Cortaid / Delacort / Ficortril / Genacort / Glycort / Komed HC / Lacticare HC / Lubricort / Meusicort / Mildison / Nogenic HC / Nutracort / Penecort / Permicort / Polcort H / Preparation H Hydrocortisone Cream / Prevex HC / Proctocream / Remederm HC / Sanatison / Scalpicin Capilar / Schericur / Sigmacort / Synacort / Systral Hydrocort / Timocort

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Alkindi		2.0 mg	Oral	Diurnal Europe B.V.	2021-01-22	Not applicable
Alkindi		1.0 mg	Oral	Diurnal Europe B.V.	2021-01-22	Not applicable
Alkindi		5.0 mg	Oral	Diurnal Europe B.V.	2021-01-22	Not applicable
Alkindi		0.5 mg	Oral	Diurnal Europe B.V.	2021-01-22	Not applicable
Alkindi Sprinkle	Granule	1 mg/1	Oral	Eton Pharmaceuticals, Inc.	2020-09-29	Not applicable

Generic Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Ala-Scalp	Lotion	20 mg/1mL	Topical	Lifsa Drugs Llc	2021-02-05	Not applicable
Ala-Scalp	Lotion	20 mg/1mL	Topical	Derm Ventures LLC	2020-07-24	Not applicable
Alacort	Cream	25 mg/1g	Topical	Crown Laboratories	2016-01-06	Not applicable
Alacort	Cream	10 mg/1g	Topical	Crown Laboratories	1973-03-09	Not applicable
Anusol HC	Cream	25 mg/1g	Topical	Salix Pharmaceuticals, Inc	1984-06-06	Not applicable

Over the Counter Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
1% Hydrocortisone	Cream	1 g/100g	Topical	Yuyao Jessie Commodity Co.,Ltd.	2015-12-01	Not applicable
999 Itch Relieving	Ointment	1 g/100g	Topical	Guangdong CR. Shunfeng Pharmaceutical Co Ltd	1989-07-20	Not applicable
999 Itch Relieving	Ointment	1 g/100g	Topical	Guangdong CR. Shunfeng Pharmaceutical Co Ltd	1989-07-20	Not applicable
Advanced Hydrocortisone	Cream	10 mg/1g	Topical	Ultra Seal Corporation	2011-04-05	2024-07-01
AFASSCO 1% Hydrocortisone	Ointment	0.01 g/1g	Topical	Afassco Inc.	2018-12-07	Not applicable

Mixture Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End
Acetasol HC	Hydrocortisone (1.1 g/100mL) + Acetic acid (2.41 g/100mL)	Solution	Auricular (otic)	Actavis Pharma, Inc.	2002-09-10	2017-05-31
Acetasol HC	Hydrocortisone (1.1 g/100mL) + Acetic acid (2.41 g/100mL)	Solution	Auricular (otic)	Physicians Total Care, Inc.	1994-12-15	2012-06-30
Activir Duo 50 mg/g + 10 mg/g Creme	Hydrocortisone (10 mg/g) + Acyclovir (50 mg/g)	Cream	Topical	Gsk Gebro Consumer Healthcare Gmb H	2010-02-09	Not applicable
Alumier MD Post Procedure Kit with Hydrocortisone	Hydrocortisone (10 mg/1mL) + Titanium dioxide (70 mg/1mL) + Zinc oxide (62.8 mg/1mL)	Kit	Topical	Alumier Labs	2022-03-22	Not applicable
Antibiotic Ear (Neo/Polym/HC)	Hydrocortisone (10 mg/1mL) + Neomycin sulfate (3.5 mg/1mL) + Polymyxin B sulfate (10000 [USP'U]/1mL)	Solution / drops	Auricular (otic)	Physicians Total Care, Inc.	1995-12-29	Not applicable

Unapproved/Other Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End
141016 Hydrocortisone 0.5% / Hydroquinone 4% / Tretinoin 0.025%	Hydrocortisone (0.5 g/100g) + Hydroquinone (4 g/100g) + Tretinoin (0.025 g/100g)	Emulsion	Topical	Sincerus Florida, LLC	2020-07-02	Not applicable
141017 Hydrocortisone 0.5% / Hydroquinone 6% / Tretinoin 0.025%	Hydrocortisone (0.5 g/100g) + Hydroquinone (6 g/100g) + Tretinoin (0.025 g/100g)	Emulsion	Topical	Sincerus Florida, LLC	2020-07-02	Not applicable
141060 Hydrocortisone 0.5% / Hydroquinone 4% / Tretinoin 0.025%	Hydrocortisone (0.5 g/100g) + Hydroquinone (4 g/100g) + Tretinoin (0.025 g/100g)	Emulsion	Topical	Sincerus Florida, LLC	2020-07-02	Not applicable
141061 Hydrocortisone 0.5% / Hydroquinone 8% / Tretinoin 0.025%	Hydrocortisone (0.5 g/100g) + Hydroquinone (8 g/100g) + Tretinoin (0.025 g/100g)	Emulsion	Topical	Sincerus Florida, LLC	2020-07-02	Not applicable
Ala Quin	Hydrocortisone (5 mg/1g) + Clioquinol (30 mg/1g)	Cream	Topical	Crown Laboratories	1970-08-19	2021-11-30

Chemical Identifiers

UNII: WI4X0X7BPJ
CAS number: 50-23-7
InChI Key: JYGXADMDTFJGBT-VWUMJDOOSA-N
InChI: InChI=1S/C21H30O5/c1-19-7-5-13(23)9-12(19)3-4-14-15-6-8-21(26,17(25)11-22)20(15,2)10-16(24)18(14)19/h9,14-16,18,22,24,26H,3-8,10-11H2,1-2H3/t14-,15-,16-,18+,19-,20-,21-/m0/s1
IUPAC Name: (1R,3aS,3bS,9aR,9bS,10S,11aS)-1,10-dihydroxy-1-(2-hydroxyacetyl)-9a,11a-dimethyl-1H,2H,3H,3aH,3bH,4H,5H,7H,8H,9H,9aH,9bH,10H,11H,11aH-cyclopenta[a]phenanthren-7-one
SMILES: [H][C@@]12CC[C@](O)(C(=O)CO)[C@@]1(C)C[C@H](O)[C@@]1([H])[C@@]2([H])CCC2=CC(=O)CC[C@]12C

References

Synthesis Reference

Manfred Baumgarth, Dieter Orth, Jurgen Harting, Hans Schaefer, Achim Zesch, "Hydrocortisone orthoesters, pharmaceutical formulations thereof and processes for the preparation thereof." U.S. Patent US4264584, issued March, 1974.

US4264584

General References

Werumeus Buning J, Touw DJ, Brummelman P, Dullaart RPF, van den Berg G, van der Klauw MM, Kamp J, Wolffenbuttel BHR, van Beek AP: Pharmacokinetics of oral hydrocortisone - Results and implications from a randomized controlled trial. Metabolism. 2017 Jun;71:7-16. doi: 10.1016/j.metabol.2017.02.005. Epub 2017 Feb 13. [Article]
Aalto-Korte K, Turpeinen M: Pharmacokinetics of topical hydrocortisone at plasma level after applications once or twice daily in patients with widespread dermatitis. Br J Dermatol. 1995 Aug;133(2):259-63. doi: 10.1111/j.1365-2133.1995.tb02625.x. [Article]
Aalto-Korte K, Turpeinen M: Quantifying systemic absorption of topical hydrocortisone in erythroderma. Br J Dermatol. 1995 Sep;133(3):403-8. doi: 10.1111/j.1365-2133.1995.tb02668.x. [Article]
Lima JJ, Jusko WJ: Bioavailability of hydrocortisone retention enemas in relation to absorption kinetics. Clin Pharmacol Ther. 1980 Aug;28(2):262-9. doi: 10.1038/clpt.1980.159. [Article]
FLORINI JR, BUYSKE DA: Plasma protein binding of triamcinolone-H3 and hydrocortisone-4-C14. J Biol Chem. 1961 Jan;236:247-51. [Article]
Derendorf H, Mollmann H, Barth J, Mollmann C, Tunn S, Krieg M: Pharmacokinetics and oral bioavailability of hydrocortisone. J Clin Pharmacol. 1991 May;31(5):473-6. doi: 10.1002/j.1552-4604.1991.tb01906.x. [Article]
Jung C, Greco S, Nguyen HH, Ho JT, Lewis JG, Torpy DJ, Inder WJ: Plasma, salivary and urinary cortisol levels following physiological and stress doses of hydrocortisone in normal volunteers. BMC Endocr Disord. 2014 Nov 26;14:91. doi: 10.1186/1472-6823-14-91. [Article]
Ciriaco M, Ventrice P, Russo G, Scicchitano M, Mazzitello G, Scicchitano F, Russo E: Corticosteroid-related central nervous system side effects. J Pharmacol Pharmacother. 2013 Dec;4(Suppl 1):S94-8. doi: 10.4103/0976-500X.120975. [Article]
Simoni R, Hill R, Vaughan M: The Isolation of Thyroxine and Cortisone: the Work of Edward C. Kendall Journal of Biological Chemistry. 2002 May 24;277(21):e10. [Article]
Yasir M, Sonthalia S: Corticosteroid Adverse Effects . [Article]
Gardill BR, Vogl MR, Lin HY, Hammond GL, Muller YA: Corticosteroid-binding globulin: structure-function implications from species differences. PLoS One. 2012;7(12):e52759. doi: 10.1371/journal.pone.0052759. Epub 2012 Dec 26. [Article]
Czock D, Keller F, Rasche FM, Haussler U: Pharmacokinetics and pharmacodynamics of systemically administered glucocorticoids. Clin Pharmacokinet. 2005;44(1):61-98. doi: 10.2165/00003088-200544010-00003. [Article]
Sarkar U, Rivera-Burgos D, Large EM, Hughes DJ, Ravindra KC, Dyer RL, Ebrahimkhani MR, Wishnok JS, Griffith LG, Tannenbaum SR: Metabolite profiling and pharmacokinetic evaluation of hydrocortisone in a perfused three-dimensional human liver bioreactor. Drug Metab Dispos. 2015 Jul;43(7):1091-9. doi: 10.1124/dmd.115.063495. Epub 2015 Apr 29. [Article]
FDA Approved Drug Products: Vosol Hydrocortisone and Glacial Acetic Acid Otic Drops [Link]
FDA Approved Drug Products: Casporyn Neomycin Sulfate, Polymixin B Sulfate, and Hydrocortisone Otic Drops [Link]
FDA Approved Drug Products: Cortef Hydrocortisone Oral Tablets [Link]
FDA Approved Drug Products: Cortenema Hydrocortisone Rectal Enema [Link]
FDA Approved Drug Products: Bacitracin, Neomycin, Polymyxin B, and Hydrocortisone Topical Ointment [Link]
FDA Approved Drug Products: Xerese (Acyclovir and Hydrocortisone) Topical Cream [Link]
FDA Approved Drug Products: Hydrocortone Hydrocortisone Oral Tablets (Discontinued) [Link]
FDA Approved Drug Products: ALKINDI SPRINKLE (hydrocortisone) oral granules [Link]

External Links

Human Metabolome Database: HMDB0000063
KEGG Drug: D00088
KEGG Compound: C00735
PubChem Compound: 5754
PubChem Substance: 46505089
ChemSpider: 5551
BindingDB: 13775
RxNav: 5492
ChEBI: 17650
ChEMBL: CHEMBL389621
ZINC: ZINC000013540519
Therapeutic Targets Database: DAP000718
PharmGKB: PA449905
Guide to Pharmacology: GtP Drug Page
PDBe Ligand: HCY
RxList: RxList Drug Page
Drugs.com: Drugs.com Drug Page
PDRhealth: PDRhealth Drug Page
Wikipedia: Hydrocortisone

PDB Entries

2v95 / 2vdy / 4c49 / 4p6x / 5hgc / 6hgf / 6hgg / 6itp / 6itq / 6nwl …

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FDA label

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MSDS

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Not Available	Available	Not Available	Acute Leukemia / Brain Neoplasm / Breast Cancer / Cancer / Desmoplastic Round Cell Sarcoma / Esophageal Andeocarcinoma / Gastric Cancer / High Grade Glioma: Glioblastoma (GBM) / Hodgkin's Lymphoma / Mixed Phenotype AML / Non-Hodgkin's Lymphoma (NHL) / Ovarian Cancer / Pancreatic Cancer / Prostate Cancer / Sarcoma, Spindle Cell / Solid Tumors / Squamous Cell Carcinoma (SCC)	1	somestatus	stop reason	just information to hide
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Not Available	Completed	Not Available	Cardiac Arrest / Infection	1	somestatus	stop reason	just information to hide
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Pharmacoeconomics

Manufacturers

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Pfizer global research development
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Mallinckrodt Inc.
Martin Surgical Supply
Meda AB
Mikart Inc.
Murfreesboro Pharmaceutical Nursing Supply
National Vitamin Company
Nexgen Pharma Inc.
Nycomed Inc.
Paddock Labs
Palmetto Pharmaceuticals Inc.
Patheon Inc.
Perrigo Co.
Person & Covey
Pfizer Inc.
Pharmacia Inc.
Pharmaderm
Pharmedix
Physician Partners Ltd.
Physicians Total Care Inc.
Preferred Pharmaceuticals Inc.
Professional Co.
Prometic Pharma Inc.
Qualitest
Ranbaxy Laboratories
Rebel Distributors Corp.
Redpharm Drug
Resource Optimization and Innovation LLC
Rising Pharmaceuticals
River's Edge Pharmaceuticals
Rouses Point Pharmaceuticals LLC
Salix Pharmaceuticals
Sandhills Packaging Inc.
Sandoz
Sanofi-Aventis Inc.
Schwarz Pharma Inc.
Solvay Pharmaceuticals
Southwood Pharmaceuticals
Stanley Pharmaceuticals Ltd.
Stat Rx Usa
Stat Scripts LLC
Summers Labs
Suppositoria Laboratories Inc.
Taro Pharmaceuticals USA
Teva Pharmaceutical Industries Ltd.
Topiderm Inc.
Triax Pharmaceuticals LLC
UCB Pharma
United Pharmaceuticals
United Research Laboratories Inc.
Universal Laboratories Inc.
Upsher Smith Laboratories
Veratex Corp.
Vertical Pharmaceuticals Inc.
Vintage Pharmaceuticals Inc.
West-Ward Pharmaceuticals
Wockhardt Ltd.
WraSer Pharmaceuticals
Wyeth Pharmaceuticals

Dosage Forms

Form	Route	Strength
Solution	Auricular (otic)
Ointment	Topical	0.01 g/1g
Lotion	Topical	20 mg/1mL
Gel	Topical
Granule	Oral	0.5 MG
Granule	Oral	1.0 MG
Granule	Oral	2.0 MG
Granule	Oral	5.0 MG
Granule	Oral	0.5 mg/1
Granule	Oral	1 mg/1
Granule	Oral	2 mg/1
Granule	Oral	5 mg/1
Cream	Topical	0.57 g/57g
Cream	Topical	1 g/1mL
Solution	Topical	1 g/100g
Cream	Topical	.05 mg/1g
Lotion	Topical	0.01 g/1g
Ointment	Topical	1 g/100g
Cream; jelly	Topical	1 %
Cream	Topical	0.01 g/1g
Cream	Topical	0.284 g/28.4g
Suspension	Auricular (otic)
Solution	Auricular (otic)	0.2 %
Cream	Cutaneous	1.000 mg
Cream	Topical	0.5 g
Spray	Topical	10 g/1mL
Lotion	Topical
Ointment	Topical	10 mg / g
Tablet	Oral	20 mg
Enema	Rectal	100 mg / 60 mL
Enema; suspension	Rectal	100 mg / 60 mL
Ointment	Topical	100 g/1g
Cream	Topical	1.116 g
Cream		0.5 %
Tablet	Oral
Cream	Topical	5 MG/G
Lotion	Topical	0.5 g
Cream	Topical	10 mg/1g
Ointment	Topical
Suspension	Topical
Lotion	Topical	10 mg/1g
Solution / drops	Ophthalmic
Gel	Topical	1 mg/1g
Lotion	Topical	1 mg/1mL
Cream	Topical	0.5 %w/w
Kit
Lotion	Topical	0.75 g/100mL
Lotion	Topical	0.45 mg/45mL
Cream	Topical	.284 g/28.4g
Cream	Topical	.284 g/287.4g
Cream	Topical	2.5 mg/g
Cream	Topical	10 mg/g
Spray	Oral	5 mg/mL
Cream	Topical	1 g/100mL
Capsule	Oral	10 MG
Capsule	Oral	20 MG
Capsule	Oral	5 MG
Capsule, extended release	Oral	10 mg
Capsule, extended release	Oral	20 mg
Capsule, extended release	Oral	5 mg
Cream	Topical	2.5 %
Solution	Topical	2.5 %
Cream	Topical	0.25 %
Kit	Oral
Ointment	Topical	10 mg/1mL
Injection	Intramuscular; Intravenous	2 G
Injection, powder, for solution	Intravenous; Parenteral	1 G/10ML
Injection, powder, for solution	Intravenous; Parenteral	500 MG/5ML
Powder, for solution	Parenteral; Rectal; Respiratory (inhalation)	100 MG/2ML
Powder, for solution	Parenteral; Rectal; Respiratory (inhalation)	25 MG/2ML
Solution	Intravenous	100.000 mg
Solution	Parenteral	500.000 mg
Cream	Topical	0.5 g/100g
Shampoo	Topical	10.2 mg/1mL
Cream	Topical	1 % w/w
Ointment	Topical	1 % w/w
Gel	Topical	10 mg/1g
Ointment	Topical	10 mg/1g
Cream	Topical	0.59 mg/59mL
Ointment	Rectal	10 mg/1g
Stick	Topical	.01 g/1g
Cream	Topical	100000 g
Lotion	Topical	0.505 g
Cream	Rectal; Topical
Cream	Topical	2.5 mg
Cream	Topical	5 mg
Cream	Topical	10 mg
Tablet	Oral	15 mg
Tablet	Oral	2.5 mg
Spray	Oral	5 mg
Tablet	Oral	10.0 mg
Aerosol, spray	Topical	1.13 g/113g
Cream	Topical	1 mg/100g
Cream	Topical	1 h/100g
Cream	Topical	10 mg/1mL
Cream	Topical	25 mg/1g
Cream	Topical	5 mg/1g
Enema	Rectal	100 mg/60mL
Gel	Topical	1 g/100g
Liquid	Topical	10 mg/1g
Liquid	Topical	10 mg/1mL
Lotion	Topical	1 g/100.65mL
Lotion	Topical	1 g/1mL
Lotion	Topical	1.14 g/114g
Lotion	Topical	10 mg/1mL
Lotion	Topical	25 mg/1mL
Ointment	Topical	0.0102 g/1g
Ointment	Topical	25 mg/1g
Ointment	Topical	5 mg/1g
Powder	Not applicable	1 g/1g
Shampoo	Topical	1 g/100mL
Suspension	Rectal	100 mg/60mL
Tablet	Oral	10 mg/1
Tablet	Oral	20 mg/1
Tablet	Oral	5 mg/1
Emulsion	Topical
Cream	Topical	1 % w/w
Ointment	Topical	10 mg/1
Cream		2.5 %
Aerosol, spray	Topical	10 mg/1g
Cream	Topical	500 mg / 100 g
Cream	Topical	1 g / 100 g
Cream	Topical	0.5 %
Cream	Topical	5 mg / g
Cream	Topical	10 mg / g
Ointment	Topical	0.5 %
Ointment	Topical	1 %
Cream	Topical	140 mg/14g
Cream	Topical	10.2 mg/1g
Ointment	Topical	10 g/100g
Ointment		10 mg
Solution	Oral	10 mg
Emulsion	Topical	10 mg
Lotion	Topical	1 g/100mL
Gel	Topical	20 mg/1g
Gel	Topical	2 g/100g
Cream	Topical	20 mg/1g
Ointment	Topical
Ointment
Solution / drops
Solution / drops	Ophthalmic
Ointment	Ophthalmic
Spray	Topical	1 g/100g
Lotion	Topical	1.02 g/100g
Kit	Oral; Topical
Tablet, chewable	Oral; Topical
Lotion	Topical	1 g/100g
Lotion	Topical	5 mg
Cream	Topical	1 %
Kit	Topical
Cream	Cutaneous	1 %
Cream		0.1 %
Emulsion	Topical	0.1 %
Ointment		0.1 %
Solution	Topical	0.1 %
Liquid	Topical	5 mg/1mL
Liquid	Topical	9 mg/1mL
Spray	Topical	10 mg/1mL
Ointment	Topical	1.02 g/100g
Cream	Topical	1.02 g/100g
Cream	Topical	1 g/100g
Cream	Topical	0.009 g/1
Solution / drops	Conjunctival
Cream	Cutaneous	1.000 g
Spray	Topical	1 g/1g
Cream	Topical	1 g/100g
Solution / drops	Auricular (otic)
Suspension	Ophthalmic
Suspension / drops	Auricular (otic)
Ointment	Ophthalmic
Solution	Parenteral	100.00 mg
Cream
Lotion	Topical	5 mg/1g
Cream	Cutaneous	1.0000 g
Solution	Cutaneous	1.0000 g
Liquid	Auricular (otic)
Kit	Topical	20 mg/1mL
Spray	Topical	1.12 g/112g
Lipstick	Topical	0.005 g/1g
Lotion	Topical	0.025 mg/2.5mL
Tablet	Oral	5 MG
Tablet, multilayer, extended release	Oral	20 mg
Tablet, multilayer, extended release	Oral	5 mg
Cream	Topical	7.5 g/100mL
Cream	Topical	1 mg/1g
Liquid	Topical	0.28 mg/100mL
Aerosol, foam	Rectal
Ointment	Rectal
Ointment	Rectal; Topical
Injection, powder, for solution	Intravenous; Parenteral	100 MG/2ML
Cream	Topical	.01 mg/1g
Cream	Topical	0.51 g/100g
Spray	Topical	500 g/1g
Cream	Topical	1 mg/100mL
Cream	Topical	0.33 %
Ointment		0.33 %
Ointment		1 %
Cream	Topical	2.5 % w/w
Lotion	Topical	2.5 %
Aerosol, foam	Topical	10 mg/1g
Solution
Liquid	Topical	1 g/100mL
Liquid	Topical
Injection, powder, for solution	Intravenous; Parenteral
Solution	Parenteral	100.000 mg
Cream	Cutaneous	1.00 g
Spray	Oral	5 mg/g
Cream	Topical
Lotion	Topical	1 g
Emulsion	Topical	2.5 mg/g
Ointment
Solution	Topical	25 mg/1mL
Lotion	Topical	1 %
Lotion	Topical	1 mL/100mL
Solution	Parenteral	100. mg
Cream	Topical	0.5 % w/w
Shampoo	Topical	10 mg/1mL
Cream	Topical	1 g
Cream	Topical
Cream	Topical	10 mg/1L
Spray	Topical	10 g/1L
Injection	Intramuscular; Intravenous
Cream
Suppository	Rectal
Tablet	Oral	10 mg
Ointment		1 %w/w
Cream		1 %w/w

Prices

Unit description	Cost	Unit
Locoid Lipocream 0.1% Cream 60 gm Tube	335.36USD	tube
Cortifoam 90 mg Foam 15 gm Can	239.99USD	can
Locoid 0.1% Solution 60ml Bottle	233.15USD	bottle
Locoid Lipocream 0.1% Cream 45 gm Tube	200.98USD	tube
Locoid 0.1% Cream 45 gm Tube	183.83USD	tube
Locoid 0.1% Ointment 45 gm Tube	174.86USD	tube
Pandel 0.1% Cream 45 gm Tube	161.37USD	tube
Pandel 0.1% Cream 15 gm Tube	138.56USD	tube
Proctocort 1% Cream 28.35 gm Tube	127.51USD	tube
Anusol-HC 2.5% Cream 30 gm Tube	106.45USD	tube
Locoid Lipocream 0.1% Cream 15 gm Tube	85.41USD	tube
Texacort 2.5% Solution 30ml Bottle	85.41USD	bottle
Cortisporin 3.5-10000-1 Solution 10ml Bottle	84.33USD	bottle
Proctofoam HC 1-1% Foam 10 gm Can	81.9USD	can
Cortisporin 3.5-10000-1 Suspension 10ml Bottle	79.55USD	bottle
Locoid 0.1% Solution 20ml Bottle	79.28USD	bottle
Cortisporin 1% Ointment 15 gm Tube	75.09USD	tube
Locoid 0.1% Cream 15 gm Tube	67.49USD	tube
Hydrocortisone Ace-Pramoxine 2.5-1% Cream 28.35 gm Tube	64.75USD	tube
Locoid 0.1% Ointment 15 gm Tube	62.04USD	tube
Hydrocortisone Valerate 0.2% Ointment 60 gm Tube	56.74USD	tube
Hydrocortisone 2.5% Lotion 59 gm Bottle	55.61USD	bottle
Westcort 0.2% Ointment 60 gm Tube	55.0USD	tube
Cortisporin 0.5-0.5-10000 Cream 7.5 gm Tube	54.37USD	tube
Westcort 0.2% Ointment 15 gm Tube	50.99USD	tube
Hydrocortisone Butyrate 0.1% Cream 45 gm Tube	49.43USD	tube
Hydrocortisone Valerate 0.2% Ointment 45 gm Tube	48.73USD	tube
Hydrocortisone 2.5% Lotion 59ml Bottle	47.47USD	bottle
Westcort 0.2% Ointment 45 gm Tube	46.97USD	tube
Hydrocortisone Valerate 0.2% Cream 60 gm Tube	44.99USD	tube
Hydrocortisone Valerate 0.2% Cream 45 gm Tube	33.99USD	tube
Ala Scalp 2% Lotion 29.6ml Bottle	30.99USD	bottle
Hydrocortisone Valerate 0.2% Ointment 15 gm Tube	30.56USD	tube
Westcort 0.2% Cream 15 gm Tube	25.99USD	tube
Hydrocortisone Valerate 0.2% Cream 15 gm Tube	19.99USD	tube
Cortisporin eye drops	19.74USD	ml
Solu-Cortef 1 g/vial	17.55USD	vial
Hydrocortisone 1% Lotion 118ml Bottle	15.99USD	bottle
Hydrocortisone Acetate 12 25 mg Suppository Box	15.01USD	box
Hydrocortisone 2.5% Ointment 28.35 gm Tube	13.68USD	tube
Hydrocortisone 2.5% Cream 30 gm Tube	13.67USD	tube
Colocort 100 mg/60ml Enema 60ml Bottle	13.15USD	bottle
Hydrocortisone 100 mg/60ml Enema 60ml Bottle	12.6USD	bottle
Hydrocortisone 0.5% Cream 28.35 gm Tube	11.99USD	tube
Hydrocortisone 1% Cream 15 gm Tube	11.99USD	tube
Hydrocortisone 1% Cream 28 gm Tube	11.99USD	tube
Hydrocortisone Acetate 1-1% Ointment 30 gm Tube	11.99USD	tube
Solu-Cortef 500 mg/vial	10.47USD	vial
Hydrocortisone hemisucc powder	9.9USD	g
Cortifoam 10% aerosol	9.35USD	g
Hydrocortisone Sod. Succinate 1 g/vial	9.01USD	vial
Solu-cortef (pf) 250 mg vial	8.58USD	vial
Cortisporin-tc ear susp	8.3USD	ml
Cortisporin ear suspension	7.86USD	ml
Solu-Cortef 250 mg/vial	7.05USD	vial
Cortenema (100 mg/60Ml) 100 mg/enm Enema	6.96USD	enema
Proctofoam-hc foam	6.77USD	g
Cortifoam 10 % Foam	6.14USD	g
Hycort (100 mg/60Ml) 100 mg/enm Enema	5.79USD	enema
Cortamed 2.5 % Ointment	5.67USD	g
Hydrocortisone Sod. Succinate 500 mg/vial	5.34USD	vial
Hydrocortisone powder	5.19USD	g
Solu-cortef (pf) 100 mg vial	4.85USD	vial
Solu-cortef 100 mg vial	4.63USD	vial
Proctocort 1% cream	4.37USD	g
Pandel 0.1% cream	4.34USD	g
Locoid 0.1% lipocream	4.3USD	g
Solu-Cortef 100 mg/vial	4.07USD	vial
Locoid 0.1% cream	3.92USD	g
Hydrocortisone Sod. Succinate 250 mg/vial	3.56USD	vial
Hydrocortisone ss 250 mg vial	3.5USD	vial
Anusol-hc 2.5% cream	3.45USD	g
Hydrocortisone acet powder	3.15USD	g
Proctofoam	2.89USD	g
A-hydrocort 100 mg vial	2.42USD	each
Proctocream-hc 2.5% cream	2.17USD	g
Hydrocortisone Sod. Succinate 100 mg/vial	2.1USD	vial
Hydrocortisone val 0.2% cream	2.07USD	g
Hytone 2.5% cream	1.46USD	g
Hydrocortisone buty 0.1% cream	1.31USD	g
First hydrocort 10% gel	1.18USD	g
Westcort 0.2% cream	1.17USD	g
Procto-kit 1% cream	1.08USD	g
Ala-scalp hp 2% lotion	1.03USD	ml
Cortef 20 mg tablet	0.9USD	tablet
Proctosol-hc 2.5% cream	0.89USD	g
Proctozone-hc 2.5% cream	0.83USD	g
Orabase plain paste	0.77USD	g
Hydrocortisone 2.5% lotion	0.6USD	ml
Cortef 10 mg tablet	0.55USD	tablet
Orabase-b 20% gel	0.55USD	g
Hydrocortisone 2.5% cream	0.53USD	g
Hydrocortisone 10 mg tablet	0.52USD	tablet
Cortef 5 mg tablet	0.45USD	tablet
Ala-cort 1% cream	0.43USD	g
Hydrocortisone 5 mg tablet	0.38USD	tablet
Corticaine 0.5% cream	0.37USD	g
Hydrocortisone 20 mg tablet	0.32USD	tablet
Prevex Hc 1 % Occlusive Cream	0.3USD	g
Emo-Cort 2.5 % Cream	0.26USD	g
Preparation h 1% cream	0.24USD	g
Tucks hydrocortisone ointment	0.24USD	g
Emo-Cort 2.5 % Lotion	0.23USD	g
Emo-Cort Scalp 2.5 % Lotion	0.22USD	g
Colocort 100 mg enema	0.21USD	ml
Cortenema 100 mg enema	0.21USD	ml
Sarna Hc 2.5 % Lotion	0.2USD	g
Emo-Cort 1 % Cream	0.19USD	g
Balneol lotion	0.18USD	ml
Emo-Cort 1 % Lotion	0.18USD	g
Lanacort 1% cool creme	0.18USD	g
Hyderm 0.5 % Cream	0.18USD	g
Hytone 1% cream	0.17USD	g
Cortoderm Mild 0.5 % Ointment	0.15USD	g
Beta hc 1% lotion	0.14USD	ml
Cortizone-10 1% spray	0.14USD	ml
Hydroval 0.2 % Cream	0.13USD	g
Hydroval 0.2 % Ointment	0.13USD	g
Aquanil hc 1% lotion	0.12USD	ml
Hydrocortisone plus 12 1% crm	0.12USD	g
Scalpicin 3% liquid	0.12USD	ml
Slender cortisol capsule	0.12USD	capsule
Cortaid 1% spray	0.1USD	ml
Sarna Hc 1 % Lotion	0.1USD	g
Hydrocortisone 0.5% cream	0.08USD	g
Hydrocortisone 1% cream	0.08USD	g
Uniderm moisturizer	0.05USD	ml
Cortoderm Regular 1 % Ointment	0.04USD	g
Hyderm 1 % Cream	0.04USD	g

DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)
US5635497	No	1997-06-03	2014-06-03
US7378405	No	2008-05-27	2026-12-19
US7981877	No	2011-07-19	2025-01-23
USRE39264	No	2006-09-05	2016-08-02
US6514980	No	2003-02-04	2019-01-24
US7223387	No	2007-05-29	2021-07-24
US9717740	No	2017-08-01	2032-11-19
US9675559	No	2017-06-13	2033-01-10
US9649280	No	2017-05-16	2034-05-12

Properties

State

Solid

Experimental Properties

Property	Value	Source
melting point (°C)	220 °C	PhysProp
water solubility	320 mg/L (at 25 °C)	YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP	1.61	HANSCH,C ET AL. (1995)
logS	-2.97	ADME Research, USCD
Caco2 permeability	-4.66	ADME Research, USCD

Predicted Properties

Property	Value	Source
Water Solubility	0.199 mg/mL	ALOGPS
logP	1.79	ALOGPS
logP	1.28	Chemaxon
logS	-3.3	ALOGPS
pKa (Strongest Acidic)	12.59	Chemaxon
pKa (Strongest Basic)	-2.8	Chemaxon
Physiological Charge	0	Chemaxon
Hydrogen Acceptor Count	5	Chemaxon
Hydrogen Donor Count	3	Chemaxon
Polar Surface Area	94.83 Å²	Chemaxon
Rotatable Bond Count	2	Chemaxon
Refractivity	97.4 m³·mol^-1	Chemaxon
Polarizability	39.45 Å³	Chemaxon
Number of Rings	4	Chemaxon
Bioavailability	1	Chemaxon
Rule of Five	Yes	Chemaxon
Ghose Filter	Yes	Chemaxon
Veber's Rule	No	Chemaxon
MDDR-like Rule	No	Chemaxon

Predicted ADMET Features

Property	Value	Probability
Human Intestinal Absorption	+	0.9918
Blood Brain Barrier	+	0.9383
Caco-2 permeable	-	0.5096
P-glycoprotein substrate	Substrate	0.7861
P-glycoprotein inhibitor I	Non-inhibitor	0.7847
P-glycoprotein inhibitor II	Non-inhibitor	0.8383
Renal organic cation transporter	Non-inhibitor	0.7463
CYP450 2C9 substrate	Non-substrate	0.8496
CYP450 2D6 substrate	Non-substrate	0.9138
CYP450 3A4 substrate	Substrate	0.7407
CYP450 1A2 substrate	Non-inhibitor	0.9406
CYP450 2C9 inhibitor	Non-inhibitor	0.9072
CYP450 2D6 inhibitor	Non-inhibitor	0.9418
CYP450 2C19 inhibitor	Non-inhibitor	0.9253
CYP450 3A4 inhibitor	Non-inhibitor	0.8902
CYP450 inhibitory promiscuity	Low CYP Inhibitory Promiscuity	0.9095
Ames test	Non AMES toxic	0.9132
Carcinogenicity	Non-carcinogens	0.9597
Biodegradation	Not ready biodegradable	0.925
Rat acute toxicity	1.8914 LD50, mol/kg	Not applicable
hERG inhibition (predictor I)	Weak inhibitor	0.95
hERG inhibition (predictor II)	Non-inhibitor	0.584

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)

Download (2.96 KB)

Spectra

Spectrum	Spectrum Type	Splash Key
GC-MS Spectrum - GC-MS (2 MEOX; 3 TMS)	GC-MS	splash10-0f7o-3930000000-b7b43b2fc9f20acfd20b
GC-MS Spectrum - GC-MS	GC-MS	splash10-0f7o-3930000000-b7b43b2fc9f20acfd20b
GC-MS Spectrum - GC-EI-TOF	GC-MS	splash10-052f-2910000000-2625335a031486ecb302
LC-MS/MS Spectrum - LC-ESI-qTof , Positive	LC-MS/MS	splash10-03di-0759000000-b337a46ecfd6de91776b
LC-MS/MS Spectrum - LC-ESI-qTof , Positive	LC-MS/MS	splash10-05fs-3940000000-2bf712a915c3a2c100a2
LC-MS/MS Spectrum - LC-ESI-IT , negative	LC-MS/MS	splash10-015a-0189000000-61afe49a8d4a96aae3f9
MS/MS Spectrum - Linear Ion Trap , negative	LC-MS/MS	splash10-00lu-0149000000-b95a11b27f7e7d44dd51
MS/MS Spectrum - Linear Ion Trap , negative	LC-MS/MS	splash10-001l-0019000000-4c4924e6ac472ad52886
MS/MS Spectrum - , negative	LC-MS/MS	splash10-001j-0259000000-fda4e876e9ef04015946
LC-MS/MS Spectrum - LC-ESI-QFT , positive	LC-MS/MS	splash10-03di-0009000000-cc8188e19dbdd6210b77
LC-MS/MS Spectrum - LC-ESI-QFT , positive	LC-MS/MS	splash10-07r1-1985000000-b6d756bd554367393be3
LC-MS/MS Spectrum - LC-ESI-QFT , positive	LC-MS/MS	splash10-00dj-1930000000-120dc8893cc4709c1f6b
LC-MS/MS Spectrum - LC-ESI-QFT , positive	LC-MS/MS	splash10-00dm-2910000000-d1f01e1bce5fe0108f40
LC-MS/MS Spectrum - LC-ESI-QFT , positive	LC-MS/MS	splash10-05tf-3900000000-4ffd79c22013fe5479b6
LC-MS/MS Spectrum - LC-ESI-QFT , positive	LC-MS/MS	splash10-054o-4900000000-fdbed869a0cadc21b64b
LC-MS/MS Spectrum - LC-ESI-QFT , positive	LC-MS/MS	splash10-002f-7900000000-dac7b2c5b3f8e8b85086
LC-MS/MS Spectrum - LC-ESI-QFT , positive	LC-MS/MS	splash10-016u-7900000000-3a770c3819f82ea45841
LC-MS/MS Spectrum - LC-ESI-QFT , positive	LC-MS/MS	splash10-016r-9800000000-d261cf7141fbf30715f5
MS/MS Spectrum - Linear Ion Trap , positive	LC-MS/MS	splash10-056r-0289000000-9a48511b5c3d5fa404e9
MS/MS Spectrum - , positive	LC-MS/MS	splash10-03di-0759000000-b337a46ecfd6de91776b
MS/MS Spectrum - , positive	LC-MS/MS	splash10-05fs-3940000000-2bf712a915c3a2c100a2
Predicted MS/MS Spectrum - 10V, Positive (Annotated)	Predicted LC-MS/MS	splash10-01t9-0009000000-4093ca5af0da3685f238
Predicted MS/MS Spectrum - 10V, Negative (Annotated)	Predicted LC-MS/MS	splash10-001i-0009000000-de7025f83ad3d5bbe454
Predicted MS/MS Spectrum - 20V, Positive (Annotated)	Predicted LC-MS/MS	splash10-054k-0629000000-50050ee94d788235c6dd
Predicted MS/MS Spectrum - 20V, Negative (Annotated)	Predicted LC-MS/MS	splash10-01q9-1009000000-156b042ede0b08bd0272
Predicted MS/MS Spectrum - 40V, Negative (Annotated)	Predicted LC-MS/MS	splash10-0gw3-1039000000-ba4294bc29ac2df09c71
Predicted MS/MS Spectrum - 40V, Positive (Annotated)	Predicted LC-MS/MS	splash10-05mo-0940000000-7b25c8eeb717ba66538b
Predicted 1H NMR Spectrum	1D NMR	Not Applicable
Predicted 13C NMR Spectrum	1D NMR	Not Applicable

Chromatographic Properties

Collision Cross Sections (CCS)

Adduct	CCS Value (Å²)	Source type	Source
[M-H]-	194.2512151	predicted	DarkChem Lite v0.1.0
[M-H]-	194.2854151	predicted	DarkChem Lite v0.1.0
[M-H]-	194.4778151	predicted	DarkChem Lite v0.1.0
[M-H]-	195.5972151	predicted	DarkChem Lite v0.1.0
[M-H]-	188.46715	predicted	DeepCCS 1.0 (2019)
[M+H]+	194.7928151	predicted	DarkChem Lite v0.1.0
[M+H]+	181.5477861	predicted	DarkChem Standard v0.1.0
[M+H]+	196.1118151	predicted	DarkChem Lite v0.1.0
[M+H]+	196.0463151	predicted	DarkChem Lite v0.1.0
[M+H]+	190.36255	predicted	DeepCCS 1.0 (2019)
[M+Na]+	194.2409151	predicted	DarkChem Lite v0.1.0
[M+Na]+	191.3158269	predicted	DarkChem Standard v0.1.0
[M+Na]+	195.0088151	predicted	DarkChem Lite v0.1.0
[M+Na]+	196.90793	predicted	DeepCCS 1.0 (2019)

Targets

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Property	Measurement	pH	Temperature (°C)	References
Ki (nM)	30	N/A	N/A	A29121

Details1. Glucocorticoid receptor

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Agonist

General Function: Receptor for glucocorticoids (GC) (PubMed:27120390, PubMed:37478846). Has a dual mode of action: as a transcription factor that binds to glucocorticoid response elements (GRE), both for nuclear and mitochondrial DNA, and as a modulator of other transcription factors (PubMed:28139699). Affects inflammatory responses, cellular proliferation and differentiation in target tissues. Involved in chromatin remodeling (PubMed:9590696). Plays a role in rapid mRNA degradation by binding to the 5' UTR of target mRNAs and interacting with PNRC2 in a ligand-dependent manner which recruits the RNA helicase UPF1 and the mRNA-decapping enzyme DCP1A, leading to RNA decay (PubMed:25775514). Could act as a coactivator for STAT5-dependent transcription upon growth hormone (GH) stimulation and could reveal an essential role of hepatic GR in the control of body growth (By similarity)
Specific Function: Core promoter sequence-specific dna binding
Gene Name: NR3C1
Uniprot ID: P04150
Uniprot Name: Glucocorticoid receptor
Molecular Weight: 85658.57 Da

References

Grossman R, Yehuda R, Golier J, McEwen B, Harvey P, Maria NS: Cognitive effects of intravenous hydrocortisone in subjects with PTSD and healthy control subjects. Ann N Y Acad Sci. 2006 Jul;1071:410-21. [Article]
Rautanen A, Eriksson JG, Kere J, Andersson S, Osmond C, Tienari P, Sairanen H, Barker DJ, Phillips DI, Forsen T, Kajantie E: Associations of body size at birth with late-life cortisol concentrations and glucose tolerance are modified by haplotypes of the glucocorticoid receptor gene. J Clin Endocrinol Metab. 2006 Nov;91(11):4544-51. Epub 2006 Aug 8. [Article]
Hammer F, Stewart PM: Cortisol metabolism in hypertension. Best Pract Res Clin Endocrinol Metab. 2006 Sep;20(3):337-53. [Article]
Shaw JR, Gabor K, Hand E, Lankowski A, Durant L, Thibodeau R, Stanton CR, Barnaby R, Coutermarsh B, Karlson KH, Sato JD, Hamilton JW, Stanton BA: Role of glucocorticoid receptor in acclimation of killifish (Fundulus heteroclitus) to seawater and effects of arsenic. Am J Physiol Regul Integr Comp Physiol. 2007 Feb;292(2):R1052-60. Epub 2006 Oct 12. [Article]
Sher L: Combined dexamethasone suppression-corticotropin-releasing hormone stimulation test in studies of depression, alcoholism, and suicidal behavior. ScientificWorldJournal. 2006 Oct 31;6:1398-404. [Article]
Czock D, Keller F, Rasche FM, Haussler U: Pharmacokinetics and pharmacodynamics of systemically administered glucocorticoids. Clin Pharmacokinet. 2005;44(1):61-98. doi: 10.2165/00003088-200544010-00003. [Article]

Details2. Annexin A1

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Agonist

General Function: Plays important roles in the innate immune response as effector of glucocorticoid-mediated responses and regulator of the inflammatory process. Has anti-inflammatory activity (PubMed:8425544). Plays a role in glucocorticoid-mediated down-regulation of the early phase of the inflammatory response (By similarity). Contributes to the adaptive immune response by enhancing signaling cascades that are triggered by T-cell activation, regulates differentiation and proliferation of activated T-cells (PubMed:17008549). Promotes the differentiation of T-cells into Th1 cells and negatively regulates differentiation into Th2 cells (PubMed:17008549). Has no effect on unstimulated T cells (PubMed:17008549). Negatively regulates hormone exocytosis via activation of the formyl peptide receptors and reorganization of the actin cytoskeleton (PubMed:19625660). Has high affinity for Ca(2+) and can bind up to eight Ca(2+) ions (By similarity). Displays Ca(2+)-dependent binding to phospholipid membranes (PubMed:2532504, PubMed:8557678). Plays a role in the formation of phagocytic cups and phagosomes. Plays a role in phagocytosis by mediating the Ca(2+)-dependent interaction between phagosomes and the actin cytoskeleton (By similarity)
Specific Function: Cadherin binding involved in cell-cell adhesion
Gene Name: ANXA1
Uniprot ID: P04083
Uniprot Name: Annexin A1
Molecular Weight: 38713.855 Da

References

Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
Sato-Matsumura KC, Matsumura T, Nakamura H, Sawa H, Nagashima K, Koizumi H: Membrane expression of annexin I is enhanced by calcium and TPA in cultured human keratinocytes. Arch Dermatol Res. 2000 Oct;292(10):496-9. [Article]
White MV, Igarashi Y, Lundgren JD, Shelhamer J, Kaliner M: Hydrocortisone inhibits rat basophilic leukemia cell mediator release induced by neutrophil-derived histamine releasing activity as well as by anti-IgE. J Immunol. 1991 Jul 15;147(2):667-73. [Article]
Serres M, Viac J, Comera C, Schmitt D: Expression of annexin I in freshly isolated human epidermal cells and in cultured keratinocytes. Arch Dermatol Res. 1994;286(5):268-72. [Article]

Enzymes

Property	Measurement	pH	Temperature (°C)	References
IC 50 (nM)	>50000	N/A	N/A	A15818

Details1. Cytochrome P450 3A4

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate
Inducer

General Function: A cytochrome P450 monooxygenase involved in the metabolism of sterols, steroid hormones, retinoids and fatty acids (PubMed:10681376, PubMed:11093772, PubMed:11555828, PubMed:12865317, PubMed:14559847, PubMed:15373842, PubMed:15764715, PubMed:19965576, PubMed:20702771, PubMed:21490593, PubMed:21576599). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase). Catalyzes the hydroxylation of carbon-hydrogen bonds (PubMed:12865317, PubMed:14559847, PubMed:15373842, PubMed:15764715, PubMed:21490593, PubMed:21576599, PubMed:2732228). Exhibits high catalytic activity for the formation of hydroxyestrogens from estrone (E1) and 17beta-estradiol (E2), namely 2-hydroxy E1 and E2, as well as D-ring hydroxylated E1 and E2 at the C-16 position (PubMed:11555828, PubMed:12865317, PubMed:14559847). Plays a role in the metabolism of androgens, particularly in oxidative deactivation of testosterone (PubMed:15373842, PubMed:15764715, PubMed:22773874, PubMed:2732228). Metabolizes testosterone to less biologically active 2beta- and 6beta-hydroxytestosterones (PubMed:15373842, PubMed:15764715, PubMed:2732228). Contributes to the formation of hydroxycholesterols (oxysterols), particularly A-ring hydroxylated cholesterol at the C-4beta position, and side chain hydroxylated cholesterol at the C-25 position, likely contributing to cholesterol degradation and bile acid biosynthesis (PubMed:21576599). Catalyzes bisallylic hydroxylation of polyunsaturated fatty acids (PUFA) (PubMed:9435160). Catalyzes the epoxidation of double bonds of PUFA with a preference for the last double bond (PubMed:19965576). Metabolizes endocannabinoid arachidonoylethanolamide (anandamide) to 8,9-, 11,12-, and 14,15-epoxyeicosatrienoic acid ethanolamides (EpETrE-EAs), potentially modulating endocannabinoid system signaling (PubMed:20702771). Plays a role in the metabolism of retinoids. Displays high catalytic activity for oxidation of all-trans-retinol to all-trans-retinal, a rate-limiting step for the biosynthesis of all-trans-retinoic acid (atRA) (PubMed:10681376). Further metabolizes atRA toward 4-hydroxyretinoate and may play a role in hepatic atRA clearance (PubMed:11093772). Responsible for oxidative metabolism of xenobiotics. Acts as a 2-exo-monooxygenase for plant lipid 1,8-cineole (eucalyptol) (PubMed:11159812). Metabolizes the majority of the administered drugs. Catalyzes sulfoxidation of the anthelmintics albendazole and fenbendazole (PubMed:10759686). Hydroxylates antimalarial drug quinine (PubMed:8968357). Acts as a 1,4-cineole 2-exo-monooxygenase (PubMed:11695850). Also involved in vitamin D catabolism and calcium homeostasis. Catalyzes the inactivation of the active hormone calcitriol (1-alpha,25-dihydroxyvitamin D(3)) (PubMed:29461981)
Specific Function: 1,8-cineole 2-exo-monooxygenase activity
Gene Name: CYP3A4
Uniprot ID: P08684
Uniprot Name: Cytochrome P450 3A4
Molecular Weight: 57342.67 Da

References

Ekins S, Bravi G, Wikel JH, Wrighton SA: Three-dimensional-quantitative structure activity relationship analysis of cytochrome P-450 3A4 substrates. J Pharmacol Exp Ther. 1999 Oct;291(1):424-33. [Article]
El-Sankary W, Bombail V, Gibson GG, Plant N: Glucocorticoid-mediated induction of CYP3A4 is decreased by disruption of a protein: DNA interaction distinct from the pregnane X receptor response element. Drug Metab Dispos. 2002 Sep;30(9):1029-34. [Article]
El-Sankary W, Plant NJ, Gibson GG, Moore DJ: Regulation of the CYP3A4 gene by hydrocortisone and xenobiotics: role of the glucocorticoid and pregnane X receptors. Drug Metab Dispos. 2000 May;28(5):493-6. [Article]
Abel SM, Back DJ: Cortisol metabolism in vitro--III. Inhibition of microsomal 6 beta-hydroxylase and cytosolic 4-ene-reductase. J Steroid Biochem Mol Biol. 1993 Dec;46(6):827-32. doi: 10.1016/0960-0760(93)90325-q. [Article]
Flockhart Table of Drug Interactions [Link]

Details2. Cytochrome P450 3A5

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: A cytochrome P450 monooxygenase involved in the metabolism of steroid hormones and vitamins (PubMed:10681376, PubMed:11093772, PubMed:12865317, PubMed:2732228). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase). Catalyzes the hydroxylation of carbon-hydrogen bonds (PubMed:10681376, PubMed:11093772, PubMed:12865317, PubMed:2732228). Exhibits high catalytic activity for the formation of catechol estrogens from 17beta-estradiol (E2) and estrone (E1), namely 2-hydroxy E1 and E2 (PubMed:12865317). Catalyzes 6beta-hydroxylation of the steroid hormones testosterone, progesterone, and androstenedione (PubMed:2732228). Catalyzes the oxidative conversion of all-trans-retinol to all-trans-retinal, a rate-limiting step for the biosynthesis of all-trans-retinoic acid (atRA) (PubMed:10681376). Further metabolizes all trans-retinoic acid (atRA) to 4-hydroxyretinoate and may play a role in hepatic atRA clearance (PubMed:11093772). Also involved in the oxidative metabolism of xenobiotics, including calcium channel blocking drug nifedipine and immunosuppressive drug cyclosporine (PubMed:2732228)
Specific Function: Aromatase activity
Gene Name: CYP3A5
Uniprot ID: P20815
Uniprot Name: Cytochrome P450 3A5
Molecular Weight: 57108.065 Da

References

Abel SM, Back DJ: Cortisol metabolism in vitro--III. Inhibition of microsomal 6 beta-hydroxylase and cytosolic 4-ene-reductase. J Steroid Biochem Mol Biol. 1993 Dec;46(6):827-32. doi: 10.1016/0960-0760(93)90325-q. [Article]
Flockhart Table of Drug Interactions [Link]

Details3. Cytochrome P450 3A7

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: A cytochrome P450 monooxygenase involved in the metabolism of steroid hormones and vitamins during embryogenesis (PubMed:11093772, PubMed:12865317, PubMed:14559847, PubMed:17178770, PubMed:9555064). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:11093772, PubMed:12865317, PubMed:14559847, PubMed:17178770, PubMed:9555064). Catalyzes the hydroxylation of carbon-hydrogen bonds. Metabolizes 3beta-hydroxyandrost-5-en-17-one (dehydroepiandrosterone, DHEA), a precursor in the biosynthesis of androgen and estrogen steroid hormones (PubMed:17178770, PubMed:9555064). Exhibits high catalytic activity for the formation of hydroxyestrogens from estrone (E1), particularly D-ring hydroxylated estrone at the C16-alpha position (PubMed:12865317, PubMed:14559847). Mainly hydroxylates all trans-retinoic acid (atRA) to 4-hydroxyretinoate and may play a role in atRA clearance during fetal development (PubMed:11093772). Also involved in the oxidative metabolism of xenobiotics including anticonvulsants (PubMed:9555064)
Specific Function: All-trans retinoic acid 18-hydroxylase activity
Gene Name: CYP3A7
Uniprot ID: P24462
Uniprot Name: Cytochrome P450 3A7
Molecular Weight: 57469.95 Da

References

Abel SM, Back DJ: Cortisol metabolism in vitro--III. Inhibition of microsomal 6 beta-hydroxylase and cytosolic 4-ene-reductase. J Steroid Biochem Mol Biol. 1993 Dec;46(6):827-32. doi: 10.1016/0960-0760(93)90325-q. [Article]
Flockhart Table of Drug Interactions [Link]

Details4. Cytochrome P450 11B1, mitochondrial

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: A cytochrome P450 monooxygenase involved in the biosynthesis of adrenal corticoids (PubMed:12530636, PubMed:1518866, PubMed:1775135, PubMed:18215163, PubMed:23322723). Catalyzes a variety of reactions that are essential for many species, including detoxification, defense, and the formation of endogenous chemicals like steroid hormones. Steroid 11beta, 18- and 19-hydroxylase with preferred regioselectivity at 11beta, then 18, and lastly 19 (By similarity). Catalyzes the hydroxylation of 11-deoxycortisol and 11-deoxycorticosterone (21-hydroxyprogesterone) at 11beta position, yielding cortisol or corticosterone, respectively, but cannot produce aldosterone (PubMed:12530636, PubMed:1518866, PubMed:1775135, PubMed:18215163, PubMed:23322723). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate for hydroxylation and reducing the second into a water molecule. Two electrons are provided by NADPH via a two-protein mitochondrial transfer system comprising flavoprotein FDXR (adrenodoxin/ferredoxin reductase) and nonheme iron-sulfur protein FDX1 or FDX2 (adrenodoxin/ferredoxin) (PubMed:18215163). Due to its lack of 18-oxidation activity, it is incapable of generating aldosterone (PubMed:23322723). Could also be involved in the androgen metabolic pathway (Probable)
Specific Function: Corticosterone 18-monooxygenase activity
Gene Name: CYP11B1
Uniprot ID: P15538
Uniprot Name: Cytochrome P450 11B1, mitochondrial
Molecular Weight: 57572.44 Da

References

Freel EM, Shakerdi LA, Friel EC, Wallace AM, Davies E, Fraser R, Connell JM: Studies on the origin of circulating 18-hydroxycortisol and 18-oxocortisol in normal human subjects. J Clin Endocrinol Metab. 2004 Sep;89(9):4628-33. doi: 10.1210/jc.2004-0379. [Article]

Details5. Cytochrome P450 11B2, mitochondrial

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: A cytochrome P450 monooxygenase that catalyzes the biosynthesis of aldosterone, the main mineralocorticoid in the human body responsible for salt and water homeostasis, thus involved in blood pressure regulation, arterial hypertension, and the development of heart failure (PubMed:11856349, PubMed:12530636, PubMed:1518866, PubMed:15356073, PubMed:1594605, PubMed:1775135, PubMed:22446688, PubMed:23322723, PubMed:9814482, PubMed:9814506). Catalyzes three sequential oxidative reactions of 11-deoxycorticosterone (21-hydroxyprogesterone), namely 11-beta hydroxylation, followed by two successive oxidations at C18 yielding 18-hydroxy and then 18-oxo intermediates (that would not leave the enzyme active site during the consecutive hydroxylation reactions), ending with the formation of aldosterone (PubMed:11856349, PubMed:12530636, PubMed:1518866, PubMed:1594605, PubMed:1775135, PubMed:22446688, PubMed:23322723, PubMed:9814506). Can also produce 18-hydroxycortisol and 18-oxocortisol, derived from successive oxidations of cortisol at C18, normally found at very low levels, but significantly increased in primary aldosteronism, the most common form of secondary hypertension (PubMed:15356073, PubMed:9814482). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate and reducing the second into a water molecule. Two electrons are provided by NADPH via a two-protein mitochondrial transfer system comprising flavoprotein FDXR (adrenodoxin/ferredoxin reductase) and nonheme iron-sulfur protein FDX1 or FDX2 (adrenodoxin/ferredoxin) (PubMed:11856349, PubMed:1594605, PubMed:23322723, PubMed:9814506). Could also be involved in the androgen metabolic pathway (Probable)
Specific Function: Corticosterone 18-monooxygenase activity
Gene Name: CYP11B2
Uniprot ID: P19099
Uniprot Name: Cytochrome P450 11B2, mitochondrial
Molecular Weight: 57559.62 Da

References

Freel EM, Shakerdi LA, Friel EC, Wallace AM, Davies E, Fraser R, Connell JM: Studies on the origin of circulating 18-hydroxycortisol and 18-oxocortisol in normal human subjects. J Clin Endocrinol Metab. 2004 Sep;89(9):4628-33. doi: 10.1210/jc.2004-0379. [Article]

Details6. Cytochrome P450 2C8

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inducer

General Function: A cytochrome P450 monooxygenase involved in the metabolism of various endogenous substrates, including fatty acids, steroid hormones and vitamins (PubMed:11093772, PubMed:14559847, PubMed:15766564, PubMed:19965576, PubMed:7574697). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:11093772, PubMed:14559847, PubMed:15766564, PubMed:19965576, PubMed:7574697). Primarily catalyzes the epoxidation of double bonds of polyunsaturated fatty acids (PUFA) with a preference for the last double bond (PubMed:15766564, PubMed:19965576, PubMed:7574697). Catalyzes the hydroxylation of carbon-hydrogen bonds. Metabolizes all trans-retinoic acid toward its 4-hydroxylated form (PubMed:11093772). Displays 16-alpha hydroxylase activity toward estrogen steroid hormones, 17beta-estradiol (E2) and estrone (E1) (PubMed:14559847). Plays a role in the oxidative metabolism of xenobiotics. It is the principal enzyme responsible for the metabolism of the anti-cancer drug paclitaxel (taxol) (PubMed:26427316)
Specific Function: Arachidonic acid epoxygenase activity
Gene Name: CYP2C8
Uniprot ID: P10632
Uniprot Name: Cytochrome P450 2C8
Molecular Weight: 55824.275 Da

References

Bauersachs J, Christ M, Ertl G, Michaelis UR, Fisslthaler B, Busse R, Fleming I: Cytochrome P450 2C expression and EDHF-mediated relaxation in porcine coronary arteries is increased by cortisol. Cardiovasc Res. 2002 Jun;54(3):669-75. [Article]
Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [Article]

Details7. Aldo-keto reductase family 1 member D1

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: Catalyzes the stereospecific NADPH-dependent reduction of the C4-C5 double bond of bile acid intermediates and steroid hormones carrying a delta(4)-3-one structure to yield an A/B cis-ring junction. This cis-configuration is crucial for bile acid biosynthesis and plays important roles in steroid metabolism. Capable of reducing a broad range of delta-(4)-3-ketosteroids from C18 (such as, 17beta-hydroxyestr-4-en-3-one) to C27 (such as, 7alpha-hydroxycholest-4-en-3-one)
Specific Function: Aldo-keto reductase (nadph) activity
Gene Name: AKR1D1
Uniprot ID: P51857
Uniprot Name: Aldo-keto reductase family 1 member D1
Molecular Weight: 37376.615 Da

References

Finken MJ, Andrews RC, Andrew R, Walker BR: Cortisol metabolism in healthy young adults: sexual dimorphism in activities of A-ring reductases, but not 11beta-hydroxysteroid dehydrogenases. J Clin Endocrinol Metab. 1999 Sep;84(9):3316-21. doi: 10.1210/jcem.84.9.6009. [Article]

Details8. 3-oxo-5-alpha-steroid 4-dehydrogenase 2

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: Converts testosterone (T) into 5-alpha-dihydrotestosterone (DHT) and progesterone or corticosterone into their corresponding 5-alpha-3-oxosteroids. It plays a central role in sexual differentiation and androgen physiology
Specific Function: 3-oxo-5-alpha-steroid 4-dehydrogenase activity
Gene Name: SRD5A2
Uniprot ID: P31213
Uniprot Name: 3-oxo-5-alpha-steroid 4-dehydrogenase 2
Molecular Weight: 28407.035 Da

References

Finken MJ, Andrews RC, Andrew R, Walker BR: Cortisol metabolism in healthy young adults: sexual dimorphism in activities of A-ring reductases, but not 11beta-hydroxysteroid dehydrogenases. J Clin Endocrinol Metab. 1999 Sep;84(9):3316-21. doi: 10.1210/jcem.84.9.6009. [Article]

Details9. 11-beta-hydroxysteroid dehydrogenase type 2

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: Catalyzes the conversion of biologically active 11beta-hydroxyglucocorticoids (11beta-hydroxysteroid) such as cortisol, to inactive 11-ketoglucocorticoids (11-oxosteroid) such as cortisone, in the presence of NAD(+) (PubMed:10497248, PubMed:12788846, PubMed:17314322, PubMed:22796344, PubMed:27927697, PubMed:30902677, PubMed:33387577, PubMed:7859916, PubMed:8538347). Functions as a dehydrogenase (oxidase), thereby decreasing the concentration of active glucocorticoids, thus protecting the nonselective mineralocorticoid receptor from occupation by glucocorticoids (PubMed:10497248, PubMed:12788846, PubMed:17314322, PubMed:33387577, PubMed:7859916). Plays an important role in maintaining glucocorticoids balance during preimplantation and protects the fetus from excessive maternal corticosterone exposure (By similarity). Catalyzes the oxidation of 11beta-hydroxytestosterone (11beta,17beta-dihydroxyandrost-4-ene-3-one) to 11-ketotestosterone (17beta-hydroxyandrost-4-ene-3,11-dione), a major bioactive androgen (PubMed:22796344, PubMed:27927697). Catalyzes the conversion of 11beta-hydroxyandrostenedione (11beta-hydroxyandrost-4-ene-3,17-dione) to 11-ketoandrostenedione (androst-4-ene-3,11,17-trione), which can be further metabolized to 11-ketotestosterone (PubMed:27927697). Converts 7-beta-25-dihydroxycholesterol to 7-oxo-25-hydroxycholesterol in vitro (PubMed:30902677). 7-beta-25-dihydroxycholesterol (not 7-oxo-25-hydroxycholesterol) acts as a ligand for the G-protein-coupled receptor (GPCR) Epstein-Barr virus-induced gene 2 (EBI2) and may thereby regulate immune cell migration (PubMed:30902677). May protect ovulating oocytes and fertilizing spermatozoa from the adverse effects of cortisol (By similarity)
Specific Function: 11-beta-hydroxysteroid dehydrogenase (nad+) activity
Gene Name: HSD11B2
Uniprot ID: P80365
Uniprot Name: 11-beta-hydroxysteroid dehydrogenase type 2
Molecular Weight: 44126.06 Da

References

Finken MJ, Andrews RC, Andrew R, Walker BR: Cortisol metabolism in healthy young adults: sexual dimorphism in activities of A-ring reductases, but not 11beta-hydroxysteroid dehydrogenases. J Clin Endocrinol Metab. 1999 Sep;84(9):3316-21. doi: 10.1210/jcem.84.9.6009. [Article]
Sarkar U, Rivera-Burgos D, Large EM, Hughes DJ, Ravindra KC, Dyer RL, Ebrahimkhani MR, Wishnok JS, Griffith LG, Tannenbaum SR: Metabolite profiling and pharmacokinetic evaluation of hydrocortisone in a perfused three-dimensional human liver bioreactor. Drug Metab Dispos. 2015 Jul;43(7):1091-9. doi: 10.1124/dmd.115.063495. Epub 2015 Apr 29. [Article]

Details10. 11-beta-hydroxysteroid dehydrogenase 1

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: Controls the reversible conversion of biologically active glucocorticoids such as cortisone to cortisol, and 11-dehydrocorticosterone to corticosterone in the presence of NADP(H) (PubMed:10497248, PubMed:12460758, PubMed:14973125, PubMed:15152005, PubMed:15280030, PubMed:17593962, PubMed:21453287, PubMed:27927697, PubMed:30902677). Participates in the corticosteroid receptor-mediated anti-inflammatory response, as well as metabolic and homeostatic processes (PubMed:10497248, PubMed:12414862, PubMed:15152005, PubMed:21453287). Plays a role in the secretion of aqueous humor in the eye, maintaining a normotensive, intraocular environment (PubMed:11481269). Bidirectional in vitro, predominantly functions as a reductase in vivo, thereby increasing the concentration of active glucocorticoids (PubMed:10497248, PubMed:11481269, PubMed:12414862, PubMed:12460758). It has broad substrate specificity, besides glucocorticoids, it accepts other steroid and sterol substrates (PubMed:15095019, PubMed:15152005, PubMed:17593962, PubMed:21453287). Interconverts 7-oxo- and 7-hydroxy-neurosteroids such as 7-oxopregnenolone and 7beta-hydroxypregnenolone, 7-oxodehydroepiandrosterone (3beta-hydroxy-5-androstene-7,17-dione) and 7beta-hydroxydehydroepiandrosterone (3beta,7beta-dihydroxyandrost-5-en-17-one), among others (PubMed:17593962). Catalyzes the stereo-specific conversion of the major dietary oxysterol, 7-ketocholesterol (7-oxocholesterol), into the more polar 7-beta-hydroxycholesterol metabolite (PubMed:15095019, PubMed:15152005). 7-oxocholesterol is one of the most important oxysterols, it participates in several events such as induction of apoptosis, accumulation in atherosclerotic lesions, lipid peroxidation, and induction of foam cell formation (PubMed:15095019). Mediates the 7-oxo reduction of 7-oxolithocholate mainly to chenodeoxycholate, and to a lesser extent to ursodeoxycholate, both in its free form and when conjugated to glycine or taurine, providing a link between glucocorticoid activation and bile acid metabolism (PubMed:21453287). Catalyzes the synthesis of 7-beta-25-dihydroxycholesterol from 7-oxo-25-hydroxycholesterol in vitro, which acts as a ligand for the G-protein-coupled receptor (GPCR) Epstein-Barr virus-induced gene 2 (EBI2) and may thereby regulate immune cell migration (PubMed:30902677)
Specific Function: 11-beta-hydroxysteroid dehydrogenase (nadp+) activity
Gene Name: HSD11B1
Uniprot ID: P28845
Uniprot Name: 11-beta-hydroxysteroid dehydrogenase 1
Molecular Weight: 32400.665 Da

References

Finken MJ, Andrews RC, Andrew R, Walker BR: Cortisol metabolism in healthy young adults: sexual dimorphism in activities of A-ring reductases, but not 11beta-hydroxysteroid dehydrogenases. J Clin Endocrinol Metab. 1999 Sep;84(9):3316-21. doi: 10.1210/jcem.84.9.6009. [Article]
Sarkar U, Rivera-Burgos D, Large EM, Hughes DJ, Ravindra KC, Dyer RL, Ebrahimkhani MR, Wishnok JS, Griffith LG, Tannenbaum SR: Metabolite profiling and pharmacokinetic evaluation of hydrocortisone in a perfused three-dimensional human liver bioreactor. Drug Metab Dispos. 2015 Jul;43(7):1091-9. doi: 10.1124/dmd.115.063495. Epub 2015 Apr 29. [Article]

Details11. Cytochrome P450 2A6

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inducer

General Function: Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Constitutes the major nicotine C-oxidase. Acts as a 1,4-cineole 2-exo-monooxygenase. Possesses low phenacetin O-deethylation activity
Specific Function: Arachidonic acid epoxygenase activity
Gene Name: CYP2A6
Uniprot ID: P11509
Uniprot Name: Cytochrome P450 2A6
Molecular Weight: 56517.005 Da

References

Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [Article]

Details12. Cytochrome P450 1B1

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inducer

General Function: A cytochrome P450 monooxygenase involved in the metabolism of various endogenous substrates, including fatty acids, steroid hormones and vitamins (PubMed:10681376, PubMed:11555828, PubMed:12865317, PubMed:15258110, PubMed:20972997). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:10681376, PubMed:11555828, PubMed:12865317, PubMed:15258110, PubMed:20972997). Exhibits catalytic activity for the formation of hydroxyestrogens from estrone (E1) and 17beta-estradiol (E2), namely 2- and 4-hydroxy E1 and E2. Displays a predominant hydroxylase activity toward E2 at the C-4 position (PubMed:11555828, PubMed:12865317). Metabolizes testosterone and progesterone to B or D ring hydroxylated metabolites (PubMed:10426814). May act as a major enzyme for all-trans retinoic acid biosynthesis in extrahepatic tissues. Catalyzes two successive oxidative transformation of all-trans retinol to all-trans retinal and then to the active form all-trans retinoic acid (PubMed:10681376, PubMed:15258110). Catalyzes the epoxidation of double bonds of certain PUFA. Converts arachidonic acid toward epoxyeicosatrienoic acid (EpETrE) regioisomers, 8,9-, 11,12-, and 14,15- EpETrE, that function as lipid mediators in the vascular system (PubMed:20972997). Additionally, displays dehydratase activity toward oxygenated eicosanoids hydroperoxyeicosatetraenoates (HpETEs). This activity is independent of cytochrome P450 reductase, NADPH, and O2 (PubMed:21068195). Also involved in the oxidative metabolism of xenobiotics, particularly converting polycyclic aromatic hydrocarbons and heterocyclic aryl amines procarcinogens to DNA-damaging products (PubMed:10426814). Plays an important role in retinal vascular development. Under hyperoxic O2 conditions, promotes retinal angiogenesis and capillary morphogenesis, likely by metabolizing the oxygenated products generated during the oxidative stress. Also, contributes to oxidative homeostasis and ultrastructural organization and function of trabecular meshwork tissue through modulation of POSTN expression (By similarity)
Specific Function: Aromatase activity
Gene Name: CYP1B1
Uniprot ID: Q16678
Uniprot Name: Cytochrome P450 1B1
Molecular Weight: 60845.33 Da

References

Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [Article]

Details13. Cytochrome P450 2B6

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inducer

General Function: A cytochrome P450 monooxygenase involved in the metabolism of endocannabinoids and steroids (PubMed:12865317, PubMed:21289075). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase). Catalyzes the epoxidation of double bonds of arachidonoylethanolamide (anandamide) to 8,9-, 11,12-, and 14,15-epoxyeicosatrienoic acid ethanolamides (EpETrE-EAs), potentially modulating endocannabinoid system signaling (PubMed:21289075). Hydroxylates steroid hormones, including testosterone at C-16 and estrogens at C-2 (PubMed:12865317, PubMed:21289075). Plays a role in the oxidative metabolism of xenobiotics, including plant lipids and drugs (PubMed:11695850, PubMed:22909231). Acts as a 1,4-cineole 2-exo-monooxygenase (PubMed:11695850)
Specific Function: Anandamide 11,12 epoxidase activity
Gene Name: CYP2B6
Uniprot ID: P20813
Uniprot Name: Cytochrome P450 2B6
Molecular Weight: 56277.81 Da

References

Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [Article]

Details14. Cytochrome P450 2C9

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inducer

General Function: A cytochrome P450 monooxygenase involved in the metabolism of various endogenous substrates, including fatty acids and steroids (PubMed:12865317, PubMed:15766564, PubMed:19965576, PubMed:21576599, PubMed:7574697, PubMed:9435160, PubMed:9866708). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:12865317, PubMed:15766564, PubMed:19965576, PubMed:21576599, PubMed:7574697, PubMed:9435160, PubMed:9866708). Catalyzes the epoxidation of double bonds of polyunsaturated fatty acids (PUFA) (PubMed:15766564, PubMed:19965576, PubMed:7574697, PubMed:9866708). Catalyzes the hydroxylation of carbon-hydrogen bonds. Metabolizes cholesterol toward 25-hydroxycholesterol, a physiological regulator of cellular cholesterol homeostasis (PubMed:21576599). Exhibits low catalytic activity for the formation of catechol estrogens from 17beta-estradiol (E2) and estrone (E1), namely 2-hydroxy E1 and E2 (PubMed:12865317). Catalyzes bisallylic hydroxylation and hydroxylation with double-bond migration of polyunsaturated fatty acids (PUFA) (PubMed:9435160, PubMed:9866708). Also metabolizes plant monoterpenes such as limonene. Oxygenates (R)- and (S)-limonene to produce carveol and perillyl alcohol (PubMed:11950794). Contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenytoin, tolbutamide and losartan (PubMed:25994031)
Specific Function: (r)-limonene 6-monooxygenase activity
Gene Name: CYP2C9
Uniprot ID: P11712
Uniprot Name: Cytochrome P450 2C9
Molecular Weight: 55627.365 Da

References

Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [Article]

Details15. Cytochrome P450 2C19

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inducer

General Function: A cytochrome P450 monooxygenase involved in the metabolism of polyunsaturated fatty acids (PUFA) (PubMed:18577768, PubMed:19965576, PubMed:20972997). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:18577768, PubMed:19965576, PubMed:20972997). Catalyzes the hydroxylation of carbon-hydrogen bonds. Hydroxylates PUFA specifically at the omega-1 position (PubMed:18577768). Catalyzes the epoxidation of double bonds of PUFA (PubMed:19965576, PubMed:20972997). Also metabolizes plant monoterpenes such as limonene. Oxygenates (R)- and (S)-limonene to produce carveol and perillyl alcohol (PubMed:11950794). Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine. Hydroxylates fenbendazole at the 4' position (PubMed:23959307)
Specific Function: (r)-limonene 6-monooxygenase activity
Gene Name: CYP2C19
Uniprot ID: P33261
Uniprot Name: Cytochrome P450 2C19
Molecular Weight: 55944.565 Da

References

Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [Article]

Carriers

Property	Measurement	pH	Temperature (°C)	References
Kd (nM)	631	N/A	N/A	A27953

Details1. Sex hormone-binding globulin

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Binder

General Function: Functions as an androgen transport protein, but may also be involved in receptor mediated processes. Each dimer binds one molecule of steroid. Specific for 5-alpha-dihydrotestosterone, testosterone, and 17-beta-estradiol. Regulates the plasma metabolic clearance rate of steroid hormones by controlling their plasma concentration
Specific Function: Androgen binding
Gene Name: SHBG
Uniprot ID: P04278
Uniprot Name: Sex hormone-binding globulin
Molecular Weight: 43778.755 Da

References

Khoromi S, Muniyappa R, Nackers L, Gray N, Baldwin H, Wong KA, Matheny LA, Moquin B, Rainer A, Hill S, Remaley A, Johnson LL, Max MB, Blackman MR: Effects of chronic osteoarthritis pain on neuroendocrine function in men. J Clin Endocrinol Metab. 2006 Nov;91(11):4313-8. Epub 2006 Aug 15. [Article]
Stroud LR, Solomon C, Shenassa E, Papandonatos G, Niaura R, Lipsitt LP, Lewinn K, Buka SL: Long-term stability of maternal prenatal steroid hormones from the National Collaborative Perinatal Project: still valid after all these years. Psychoneuroendocrinology. 2007 Feb;32(2):140-50. Epub 2007 Jan 31. [Article]
Lombardi G, Mondaini N, Macchiarella A, Del Popolo G: Female sexual dysfunction and hormonal status in spinal cord injured (SCI) patients. J Androl. 2007 Sep-Oct;28(5):722-6. Epub 2007 May 9. [Article]
Shifren JL, Desindes S, McIlwain M, Doros G, Mazer NA: A randomized, open-label, crossover study comparing the effects of oral versus transdermal estrogen therapy on serum androgens, thyroid hormones, and adrenal hormones in naturally menopausal women. Menopause. 2007 Nov-Dec;14(6):985-94. [Article]
Rizzo L, Dobrovsky V, Danilowicz K, Kral M, Cross G, Serra HA, Bruno OD: Low-dose glucocorticoids in hyperandrogenism. Medicina (B Aires). 2007;67(3):247-52. [Article]
Gardill BR, Vogl MR, Lin HY, Hammond GL, Muller YA: Corticosteroid-binding globulin: structure-function implications from species differences. PLoS One. 2012;7(12):e52759. doi: 10.1371/journal.pone.0052759. Epub 2012 Dec 26. [Article]

Details2. Corticosteroid-binding globulin

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Binder

General Function: Major transport protein for glucocorticoids and progestins in the blood of almost all vertebrate species
Specific Function: Serine-type endopeptidase inhibitor activity
Gene Name: SERPINA6
Uniprot ID: P08185
Uniprot Name: Corticosteroid-binding globulin
Molecular Weight: 45140.49 Da

References

Henley DE, Lightman SL: New insights into corticosteroid-binding globulin and glucocorticoid delivery. Neuroscience. 2011 Apr 28;180:1-8. doi: 10.1016/j.neuroscience.2011.02.053. Epub 2011 Mar 1. [Article]
Czock D, Keller F, Rasche FM, Haussler U: Pharmacokinetics and pharmacodynamics of systemically administered glucocorticoids. Clin Pharmacokinet. 2005;44(1):61-98. doi: 10.2165/00003088-200544010-00003. [Article]

Transporters

Property	Measurement	pH	Temperature (°C)	References
IC 50 (nM)	>50000	N/A	N/A	A15818

Details1. ATP-dependent translocase ABCB1

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate
Inducer

General Function: Translocates drugs and phospholipids across the membrane (PubMed:2897240, PubMed:35970996, PubMed:8898203, PubMed:9038218). Catalyzes the flop of phospholipids from the cytoplasmic to the exoplasmic leaflet of the apical membrane. Participates mainly to the flop of phosphatidylcholine, phosphatidylethanolamine, beta-D-glucosylceramides and sphingomyelins (PubMed:8898203). Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells (PubMed:2897240, PubMed:35970996, PubMed:9038218)
Specific Function: Abc-type xenobiotic transporter activity
Gene Name: ABCB1
Uniprot ID: P08183
Uniprot Name: ATP-dependent translocase ABCB1
Molecular Weight: 141477.255 Da

References

Schwab D, Fischer H, Tabatabaei A, Poli S, Huwyler J: Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. J Med Chem. 2003 Apr 24;46(9):1716-25. [Article]
Kim RB, Wandel C, Leake B, Cvetkovic M, Fromm MF, Dempsey PJ, Roden MM, Belas F, Chaudhary AK, Roden DM, Wood AJ, Wilkinson GR: Interrelationship between substrates and inhibitors of human CYP3A and P-glycoprotein. Pharm Res. 1999 Mar;16(3):408-14. [Article]
Yates CR, Chang C, Kearbey JD, Yasuda K, Schuetz EG, Miller DD, Dalton JT, Swaan PW: Structural determinants of P-glycoprotein-mediated transport of glucocorticoids. Pharm Res. 2003 Nov;20(11):1794-803. [Article]
Ueda K, Okamura N, Hirai M, Tanigawara Y, Saeki T, Kioka N, Komano T, Hori R: Human P-glycoprotein transports cortisol, aldosterone, and dexamethasone, but not progesterone. J Biol Chem. 1992 Dec 5;267(34):24248-52. [Article]
Orlowski S, Mir LM, Belehradek J Jr, Garrigos M: Effects of steroids and verapamil on P-glycoprotein ATPase activity: progesterone, desoxycorticosterone, corticosterone and verapamil are mutually non-exclusive modulators. Biochem J. 1996 Jul 15;317 ( Pt 2):515-22. [Article]
Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [Article]

Details2. Solute carrier organic anion transporter family member 1A2

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inhibitor

General Function: Na(+)-independent transporter that mediates the cellular uptake of a broad range of organic anions such as the endogenous bile salts cholate and deoxycholate, either in their unconjugated or conjugated forms (taurocholate and glycocholate), at the plasmam membrane (PubMed:19129463, PubMed:7557095). Responsible for intestinal absorption of bile acids (By similarity). Transports dehydroepiandrosterone 3-sulfate (DHEAS), a major circulating steroid secreted by the adrenal cortex, as well as estrone 3-sulfate and 17beta-estradiol 17-O-(beta-D-glucuronate) (PubMed:11159893, PubMed:12568656, PubMed:19129463, PubMed:23918469, PubMed:25560245, PubMed:9539145). Mediates apical uptake of all-trans-retinol (atROL) across human retinal pigment epithelium, which is essential to maintaining the integrity of the visual cycle and thus vision (PubMed:25560245). Involved in the uptake of clinically used drugs (PubMed:17301733, PubMed:20686826, PubMed:27777271). Capable of thyroid hormone transport (both T3 or 3,3',5'-triiodo-L-thyronine, and T4 or L-tyroxine) (PubMed:19129463, PubMed:20358049). Also transports prostaglandin E2 (PubMed:19129463). Plays roles in blood-brain and -cerebrospinal fluid barrier transport of organic anions and signal mediators, and in hormone uptake by neural cells (By similarity). May also play a role in the reuptake of neuropeptides such as substance P/TAC1 and vasoactive intestinal peptide/VIP released from retinal neurons (PubMed:25132355). May play an important role in plasma and tissue distribution of the structurally diverse chemotherapeutic drugs methotrexate and paclitaxel (PubMed:23243220). Shows a pH-sensitive substrate specificity which may be ascribed to the protonation state of the binding site and leads to a stimulation of substrate transport in an acidic microenvironment (PubMed:19129463). Hydrogencarbonate/HCO3(-) acts as the probable counteranion that exchanges for organic anions (PubMed:19129463). May contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable)
Specific Function: Bile acid transmembrane transporter activity
Gene Name: SLCO1A2
Uniprot ID: P46721
Uniprot Name: Solute carrier organic anion transporter family member 1A2
Molecular Weight: 74144.105 Da

References

Kanai N, Lu R, Bao Y, Wolkoff AW, Schuster VL: Transient expression of oatp organic anion transporter in mammalian cells: identification of candidate substrates. Am J Physiol. 1996 Feb;270(2 Pt 2):F319-25. [Article]
Bossuyt X, Muller M, Hagenbuch B, Meier PJ: Polyspecific drug and steroid clearance by an organic anion transporter of mammalian liver. J Pharmacol Exp Ther. 1996 Mar;276(3):891-6. [Article]

Details3. Organic anion transporter 3

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate
Curator comments: Cortisol demonstrated substrate activity in vitro using human OAT3 expressed on Xenopus Laevis.

General Function: Functions as an organic anion/dicarboxylate exchanger that couples organic anion uptake indirectly to the sodium gradient (PubMed:14586168, PubMed:15644426, PubMed:15846473, PubMed:16455804, PubMed:31553721). Transports organic anions such as estrone 3-sulfate (E1S) and urate in exchange for dicarboxylates such as glutarate or ketoglutarate (2-oxoglutarate) (PubMed:14586168, PubMed:15846473, PubMed:15864504, PubMed:22108572, PubMed:23832370). Plays an important role in the excretion of endogenous and exogenous organic anions, especially from the kidney and the brain (PubMed:11306713, PubMed:14586168, PubMed:15846473). E1S transport is pH- and chloride-dependent and may also involve E1S/cGMP exchange (PubMed:26377792). Responsible for the transport of prostaglandin E2 (PGE2) and prostaglandin F2(alpha) (PGF2(alpha)) in the basolateral side of the renal tubule (PubMed:11907186). Involved in the transport of neuroactive tryptophan metabolites kynurenate and xanthurenate (PubMed:22108572, PubMed:23832370). Functions as a biopterin transporters involved in the uptake and the secretion of coenzymes tetrahydrobiopterin (BH4), dihydrobiopterin (BH2) and sepiapterin to urine, thereby determining baseline levels of blood biopterins (PubMed:28534121). May be involved in the basolateral transport of steviol, a metabolite of the popular sugar substitute stevioside (PubMed:15644426). May participate in the detoxification/ renal excretion of drugs and xenobiotics, such as the histamine H(2)-receptor antagonists fexofenadine and cimetidine, the antibiotic benzylpenicillin (PCG), the anionic herbicide 2,4-dichloro-phenoxyacetate (2,4-D), the diagnostic agent p-aminohippurate (PAH), the antiviral acyclovir (ACV), and the mycotoxin ochratoxin (OTA), by transporting these exogenous organic anions across the cell membrane in exchange for dicarboxylates such as 2-oxoglutarate (PubMed:11669456, PubMed:15846473, PubMed:16455804). Contributes to the renal uptake of potent uremic toxins (indoxyl sulfate (IS), indole acetate (IA), hippurate/N-benzoylglycine (HA) and 3-carboxy-4-methyl-5-propyl-2-furanpropionate (CMPF)), pravastatin, PCG, E1S and dehydroepiandrosterone sulfate (DHEAS), and is partly involved in the renal uptake of temocaprilat (an angiotensin-converting enzyme (ACE) inhibitor) (PubMed:14675047). May contribute to the release of cortisol in the adrenals (PubMed:15864504). Involved in one of the detoxification systems on the choroid plexus (CP), removes substrates such as E1S or taurocholate (TC), PCG, 2,4-D and PAH, from the cerebrospinal fluid (CSF) to the blood for eventual excretion in urine and bile (By similarity). Also contributes to the uptake of several other organic compounds such as the prostanoids prostaglandin E(2) and prostaglandin F(2-alpha), L-carnitine, and the therapeutic drugs allopurinol, 6-mercaptopurine (6-MP) and 5-fluorouracil (5-FU) (By similarity). Mediates the transport of PAH, PCG, and the statins pravastatin and pitavastatin, from the cerebrum into the blood circulation across the blood-brain barrier (BBB). In summary, plays a role in the efflux of drugs and xenobiotics, helping reduce their undesired toxicological effects on the body (By similarity)
Specific Function: Organic anion transmembrane transporter activity
Gene Name: SLC22A8
Uniprot ID: Q8TCC7
Uniprot Name: Organic anion transporter 3
Molecular Weight: 59855.585 Da

References

VanWert AL, Gionfriddo MR, Sweet DH: Organic anion transporters: discovery, pharmacology, regulation and roles in pathophysiology. Biopharm Drug Dispos. 2010 Jan;31(1):1-71. doi: 10.1002/bdd.693. [Article]

Drug created at June 13, 2005 13:24 / Updated at September 14, 2024 04:03

Hydrocortisone

Identification

Structure for Hydrocortisone (DB00741)

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Clinical Trial & Rare Diseases Add-on Data Package

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