Identification
- Summary
Deoxycholic acid is a cytolytic agent injected subcutaneously to improve the appearance submental fat.
- Brand Names
- Belkyra, Kybella
- Generic Name
- Deoxycholic acid
- DrugBank Accession Number
- DB03619
- Background
Deoxycholic acid is a a bile acid which emulsifies and solubilizes dietary fats in the intestine, and when injected subcutaneously, it disrupts cell membranes in adipocytes and destroys fat cells in that tissue. In April 2015, deoxycholic acid was approved by the FDA for the treatment submental fat to improve aesthetic appearance and reduce facial fullness or convexity. It is marketed under the brand name Kybella by Kythera Biopharma and is the first pharmacological agent available for submental fat reduction, allowing for a safer and less invasive alternative than surgical procedures.
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Deoxycholic acid (DB03619)
- Weight
- Average: 392.572
Monoisotopic: 392.292659768 - Chemical Formula
- C24H40O4
- Synonyms
- (3α,5β,12α)-3,12-dihydroxycholan-24-oic acid
- 3alpha,12alpha-Dihydroxy-5beta-cholanic acid
- 7α-deoxycholic acid
- Deoxycholate
- Deoxycholic acid
- Desoxycholic acid
- Desoxycholsäure
- External IDs
- ATX-101
Pharmacology
- Indication
For improvement in appearance of moderate to severe fullness associated with submental fat in adults.
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- Contraindications & Blackbox Warnings
Avoid life-threatening adverse drug eventsImprove clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support.- Pharmacodynamics
Not Available
- Mechanism of action
As a bile acid, deoxycholic acid emulsifies fat in the gut. Synthetically derived deoxycholic acid, when injected, stimulates a targeted breakdown of adipose cells by disrupting the cell membrane and causing adipocytolysis. This results in an inflammatory reaction and clearing of the adipose tissue remnants by macrophages. Deoxycholic acid's actions are reduced by albumin and tissue-associated proteins, therefore its effect is limited to protein-poor subcutaneous fat tissue. Protein-rich tissues like muscle and skin are unaffected by deoxycholic acid, contributing to its safety profile.
Target Actions Organism USteroid Delta-isomerase Not Available Pseudomonas putida UPpcA Not Available Geobacter sulfurreducens UElongation factor Tu GTP-binding domain-containing protein 1 Not Available Humans UCholoylglycine hydrolase Not Available Clostridium perfringens (strain 13 / Type A) ULactaldehyde dehydrogenase Not Available Escherichia coli (strain K12) UAcriflavine resistance protein B Not Available Escherichia coli (strain K12) UCytochrome c oxidase subunit 1 Not Available Rhodobacter sphaeroides UCytochrome c oxidase subunit 2 Not Available Rhodobacter sphaeroides UBile acid receptor Not Available Humans UGlutathione S-transferase P Not Available Humans UG-protein coupled bile acid receptor 1 Not Available Humans UGlutathione S-transferases (Cytosolic) inhibitorHumans - Absorption
Deoxycholic acid is rapidly absorbed after subcutaneous administration. After maximum recommended single treatment dose, 100mg, the post-treatment plasma levels returned to endogenous levels within 24 hours. With the proposed treatment guideline, no accumulation is expected.
- Volume of distribution
Not Available
- Protein binding
98%
- Metabolism
Deoxycholic acid is not metabolized to any significant extent under normal conditions.
- Route of elimination
The exogenous deoxycholic acid joins the endogenous bile acid pool in the enterohepatic circulation and is excreted unchanged in feces along with endogenous deoxycholic acid.
- Half-life
Not Available
- Clearance
Not Available
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
Not Available
- Pathways
- Not Available
- 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 Integrate drug-drug
interactions in your softwareAbciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Deoxycholic acid. Acenocoumarol The risk or severity of bleeding and bruising can be increased when Acenocoumarol is combined with Deoxycholic acid. Acetylsalicylic acid The risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Deoxycholic acid. Alteplase The risk or severity of bleeding and bruising can be increased when Alteplase is combined with Deoxycholic acid. Aluminium phosphate Aluminium phosphate can cause a decrease in the absorption of Deoxycholic acid resulting in a reduced serum concentration and potentially a decrease in efficacy. Aluminum chloride Aluminum chloride can cause a decrease in the absorption of Deoxycholic acid resulting in a reduced serum concentration and potentially a decrease in efficacy. Aluminum chlorohydrate Aluminum chlorohydrate can cause a decrease in the absorption of Deoxycholic acid resulting in a reduced serum concentration and potentially a decrease in efficacy. Aluminum hydroxide Aluminum hydroxide can cause a decrease in the absorption of Deoxycholic acid resulting in a reduced serum concentration and potentially a decrease in efficacy. Aluminum oxide Aluminum oxide can cause a decrease in the absorption of Deoxycholic acid resulting in a reduced serum concentration and potentially a decrease in efficacy. Aluminum sulfate Aluminum sulfate can cause a decrease in the absorption of Deoxycholic acid resulting in a reduced serum concentration and potentially a decrease in efficacy. 
Identify potential medication risksEasily compare up to 40 drugs with our drug interaction checker.Get severity rating, description, and management advice.Learn more - Food Interactions
- No interactions found.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Belkyra Solution 10 mg / mL Subcutaneous Abbvie 2016-01-27 Not applicable Canada 
Kybella Injection, solution 20 mg/2mL Subcutaneous Kythera Biopharmaceuticals Inc. 2015-06-08 Not applicable US 
- Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Debiline Deoxycholic acid (100 mg) + Pepsin (50 mg) Tablet Oral Lab Nadeau LtÉe, Division Of Technilab Inc. 1951-12-31 1999-09-28 Canada Debiline H Deoxycholic acid (100 mg / tab) + Homatropine methylbromide (2.5 mg / tab) + Pepsin (50 mg / tab) Tablet Oral Lab Nadeau LtÉe, Division Of Technilab Inc. 1951-12-31 1999-09-28 Canada Duchol Ect Deoxycholic acid (30 mg) + Dehydrocholic acid (30 mg) + Pancrelipase (200 mg) + Pepsin (200 mg) + Sodium taurocholate (100 mg) Tablet, delayed release Oral Duchesnay Inc. 1977-12-31 2003-07-18 Canada ENZYPLEX TABLET Deoxycholic acid (30 mg) + Cyanocobalamin (5 mcg) + Dimethicone (25 mg) + Nicotinamide (10 mg) + Pancrelipase amylase (10000 u) + Pancrelipase lipase (240 u) + Pancrelipase protease (9000 u) + Calcium pantothenate (5 mg) + Pyridoxine (5 mg) + Riboflavin (5 mg) + Thiamine (10 mg) Tablet, coated Oral ZUELLIG PHARMA PTE. LTD. 1991-03-05 Not applicable Singapore Medichol Deoxycholic acid (30 mg) + Dehydrocholic acid (30 mg) + Pancrelipase (200 mg) + Pepsin (200 mg) + Sodium taurocholate (100 mg) Tablet Oral Medic Laboratory LtÉe 1959-12-31 2007-10-22 Canada Regubil Deoxycholic acid (30 mg) + Dehydrocholic acid (30 mg) + Sodium taurocholate (150 mg) Tablet Oral Laboratoire Riva Inc 1983-12-31 Not applicable Canada
Categories
- ATC Codes
- D11AX24 — Deoxycholic acid
- Drug Categories
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as dihydroxy bile acids, alcohols and derivatives. These are compounds containing or derived from a bile acid or alcohol, and which bears exactly two carboxylic acid groups.
- Kingdom
- Organic compounds
- Super Class
- Lipids and lipid-like molecules
- Class
- Steroids and steroid derivatives
- Sub Class
- Bile acids, alcohols and derivatives
- Direct Parent
- Dihydroxy bile acids, alcohols and derivatives
- Alternative Parents
- 3-alpha-hydroxysteroids / 12-hydroxysteroids / Secondary alcohols / Cyclic alcohols and derivatives / Monocarboxylic acids and derivatives / Carboxylic acids / Organic oxides / Hydrocarbon derivatives / Carbonyl compounds
- Substituents
- 12-hydroxysteroid / 3-alpha-hydroxysteroid / 3-hydroxysteroid / Alcohol / Aliphatic homopolycyclic compound / Carbonyl group / Carboxylic acid / Carboxylic acid derivative / Cyclic alcohol / Dihydroxy bile acid, alcohol, or derivatives
- Molecular Framework
- Aliphatic homopolycyclic compounds
- External Descriptors
- bile acid, dihydroxy-5beta-cholanic acid (CHEBI:28834) / C24 bile acids, alcohols, and derivatives, Cholane and derivatives (C04483) / C24 bile acids, alcohols, and derivatives (LMST04010040)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 005990WHZZ
- CAS number
- 83-44-3
- InChI Key
- KXGVEGMKQFWNSR-LLQZFEROSA-N
- InChI
- InChI=1S/C24H40O4/c1-14(4-9-22(27)28)18-7-8-19-17-6-5-15-12-16(25)10-11-23(15,2)20(17)13-21(26)24(18,19)3/h14-21,25-26H,4-13H2,1-3H3,(H,27,28)/t14-,15-,16-,17+,18-,19+,20+,21+,23+,24-/m1/s1
- IUPAC Name
- (4R)-4-[(1R,3aS,3bR,5aR,7R,9aS,9bS,11S,11aR)-7,11-dihydroxy-9a,11a-dimethyl-hexadecahydro-1H-cyclopenta[a]phenanthren-1-yl]pentanoic acid
- SMILES
- [H][C@@]12CC[C@H]([C@H](C)CCC(O)=O)[C@@]1(C)[C@@H](O)C[C@@]1([H])[C@@]2([H])CC[C@]2([H])C[C@H](O)CC[C@]12C
References
- Synthesis Reference
Filiberto Zadini, Giorgio Zadini, "Deoxycholic acid liposome-based dermatological topical preparation." U.S. Patent US20060222695, issued October 05, 2006.
US20060222695- General References
- Wollina U, Goldman A: ATX-101 for reduction of submental fat. Expert Opin Pharmacother. 2015 Apr;16(5):755-62. doi: 10.1517/14656566.2015.1019465. Epub 2015 Feb 27. [Article]
- Walker P, Lee D: A phase 1 pharmacokinetic study of ATX-101: serum lipids and adipokines following synthetic deoxycholic acid injections. J Cosmet Dermatol. 2015 Mar;14(1):33-9. doi: 10.1111/jocd.12122. Epub 2015 Feb 14. [Article]
- FDA Approved Drug Products: KYBELLA (deoxycholic acid) injection [Link]
- External Links
- Human Metabolome Database
- HMDB0000626
- KEGG Compound
- C04483
- PubChem Compound
- 222528
- PubChem Substance
- 46506360
- ChemSpider
- 193196
- BindingDB
- 50375599
- 3194
- ChEBI
- 28834
- ChEMBL
- CHEMBL406393
- ZINC
- ZINC000003914810
- PDBe Ligand
- DXC
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Deoxycholic_acid
- PDB Entries
- 1e3v / 1fm4 / 1os6 / 2bjf / 2opx / 2w1b / 3dtu / 3o01 / 3r9v / 3rv5 … show 27 more
- FDA label
- Download (3.18 MB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Treatment Adiposity 2 4 Completed Treatment Body Fat Disorder 1 4 Completed Treatment Brassiere Strap Fat (BSF) 1 4 Completed Treatment Contour 1 4 Completed Treatment Facial Rhytides, Skin Folds, Loss of Volume and Skin Quality 1 4 Completed Treatment Fat Reduction 1 3 Completed Diagnostic Aspergillosis 1 3 Completed Other Double Chin / Healthy Subjects (HS) 1 3 Completed Treatment Efficacy / Moderate to Severe Convexity of Submental Fat / Safety 2 3 Completed Treatment Moderate or Severe Submental Fullness 6
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, solution 10 MG/ML Injection, solution 10 mg/1ml Solution Subcutaneous 10 mg / mL Injection, solution Parenteral 10 mg/ml Injection, solution Subcutaneous 10.00 mg/mL Tablet, delayed release Oral Tablet, coated Oral Injection, solution Subcutaneous 20 mg/2mL Tablet Oral Solution Subcutaneous 10 mg - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US8546367 No 2013-10-01 2028-02-21 US US7622130 No 2009-11-24 2027-12-10 US US7754230 No 2010-07-13 2027-12-10 US US8298556 No 2012-10-30 2025-08-03 US US8846066 No 2014-09-30 2025-02-08 US US8367649 No 2013-02-05 2030-03-02 US US8461140 No 2013-06-11 2028-02-21 US US8883770 No 2014-11-11 2028-02-21 US US8653058 No 2014-02-18 2030-03-02 US US8101593 No 2012-01-24 2030-03-02 US US8242294 No 2012-08-14 2028-05-16 US US9522155 No 2016-12-20 2028-02-21 US US9636349 No 2017-05-02 2028-02-21 US US9949986 No 2018-04-24 2028-02-21 US US10500214 No 2019-12-10 2030-03-02 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 177 °C PhysProp water solubility 43.6 mg/L (at 20 °C) YALKOWSKY,SH & DANNENFELSER,RM (1992) logP 3.50 RODA,A ET AL. (1990) logS -3.95 ADME Research, USCD - Predicted Properties
Property Value Source Water Solubility 0.0173 mg/mL ALOGPS logP 3.3 ALOGPS logP 3.79 Chemaxon logS -4.4 ALOGPS pKa (Strongest Acidic) 4.65 Chemaxon pKa (Strongest Basic) -0.35 Chemaxon Physiological Charge -1 Chemaxon Hydrogen Acceptor Count 4 Chemaxon Hydrogen Donor Count 3 Chemaxon Polar Surface Area 77.76 Å2 Chemaxon Rotatable Bond Count 4 Chemaxon Refractivity 109.2 m3·mol-1 Chemaxon Polarizability 46.3 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 + 0.9766 Blood Brain Barrier + 0.9288 Caco-2 permeable + 0.73 P-glycoprotein substrate Substrate 0.6648 P-glycoprotein inhibitor I Non-inhibitor 0.8737 P-glycoprotein inhibitor II Inhibitor 0.5368 Renal organic cation transporter Non-inhibitor 0.8537 CYP450 2C9 substrate Non-substrate 0.7818 CYP450 2D6 substrate Non-substrate 0.9115 CYP450 3A4 substrate Substrate 0.7407 CYP450 1A2 substrate Non-inhibitor 0.9045 CYP450 2C9 inhibitor Non-inhibitor 0.9456 CYP450 2D6 inhibitor Non-inhibitor 0.9781 CYP450 2C19 inhibitor Non-inhibitor 0.9707 CYP450 3A4 inhibitor Non-inhibitor 0.8405 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9563 Ames test Non AMES toxic 0.8794 Carcinogenicity Non-carcinogens 0.9329 Biodegradation Not ready biodegradable 0.992 Rat acute toxicity 2.5624 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9622 hERG inhibition (predictor II) Non-inhibitor 0.7246
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Targets
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- Kind
- Protein
- Organism
- Pseudomonas putida
- Pharmacological action
- Unknown
- General Function
- Steroid delta-isomerase activity
- Specific Function
- Not Available
- Gene Name
- ksi
- Uniprot ID
- P07445
- Uniprot Name
- Steroid Delta-isomerase
- Molecular Weight
- 14535.48 Da
References
- Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [Article]
- Kind
- Protein
- Organism
- Geobacter sulfurreducens
- Pharmacological action
- Unknown
- General Function
- Metal ion binding
- Specific Function
- Not Available
- Gene Name
- ppcA
- Uniprot ID
- Q8GGK7
- Uniprot Name
- Cytochrome C
- Molecular Weight
- 9747.54 Da
References
- Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Ribosome binding
- Specific Function
- Involved in the biogenesis of the 60S ribosomal subunit and translational activation of ribosomes. Together with SBDS, triggers the GTP-dependent release of EIF6 from 60S pre-ribosomes in the cytop...
- Gene Name
- EFTUD1
- Uniprot ID
- Q7Z2Z2
- Uniprot Name
- Elongation factor Tu GTP-binding domain-containing protein 1
- Molecular Weight
- 125428.745 Da
References
- Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [Article]
- Kind
- Protein
- Organism
- Clostridium perfringens (strain 13 / Type A)
- Pharmacological action
- Unknown
- General Function
- Choloylglycine hydrolase activity
- Specific Function
- The enzyme catalyzes the degradation of conjugated bile acids in the mammalian gut.
- Gene Name
- cbh
- Uniprot ID
- P54965
- Uniprot Name
- Choloylglycine hydrolase
- Molecular Weight
- 37185.0 Da
References
- Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [Article]
- Kind
- Protein
- Organism
- Escherichia coli (strain K12)
- Pharmacological action
- Unknown
- General Function
- Succinate-semialdehyde dehydrogenase [nad(p)+] activity
- Specific Function
- Acts on lactaldehyde as well as other aldehydes.
- Gene Name
- aldA
- Uniprot ID
- P25553
- Uniprot Name
- Lactaldehyde dehydrogenase
- Molecular Weight
- 52272.37 Da
References
- Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [Article]
- Kind
- Protein
- Organism
- Escherichia coli (strain K12)
- Pharmacological action
- Unknown
- General Function
- Identical protein binding
- Specific Function
- AcrA-AcrB-AcrZ-TolC is a drug efflux protein complex with broad substrate specificity that uses the proton motive force to export substrates.Involved in contact-dependent growth inhibition (CDI), a...
- Gene Name
- acrB
- Uniprot ID
- P31224
- Uniprot Name
- Multidrug efflux pump subunit AcrB
- Molecular Weight
- 113572.75 Da
References
- Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [Article]
- Kind
- Protein
- Organism
- Rhodobacter sphaeroides
- Pharmacological action
- Unknown
- General Function
- Iron ion binding
- Specific Function
- Cytochrome c oxidase is the component of the respiratory chain that catalyzes the reduction of oxygen to water. Subunits 1-3 form the functional core of the enzyme complex. Co I is the catalytic su...
- Gene Name
- ctaD
- Uniprot ID
- P33517
- Uniprot Name
- Cytochrome c oxidase subunit 1
- Molecular Weight
- 63146.395 Da
References
- Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [Article]
- Kind
- Protein
- Organism
- Rhodobacter sphaeroides
- Pharmacological action
- Unknown
- General Function
- Cytochrome-c oxidase activity
- Specific Function
- Subunits I and II form the functional core of the enzyme complex. Electrons originating in cytochrome c are transferred via heme a and Cu(A) to the binuclear center formed by heme a3 and Cu(B).
- Gene Name
- ctaC
- Uniprot ID
- Q03736
- Uniprot Name
- Cytochrome c oxidase subunit 2
- Molecular Weight
- 32930.42 Da
References
- Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Zinc ion binding
- Specific Function
- Ligand-activated transcription factor. Receptor for bile acids such as chenodeoxycholic acid, lithocholic acid and deoxycholic acid. Represses the transcription of the cholesterol 7-alpha-hydroxyla...
- Gene Name
- NR1H4
- Uniprot ID
- Q96RI1
- Uniprot Name
- Bile acid receptor
- Molecular Weight
- 55913.915 Da
References
- Fujino T, Une M, Imanaka T, Inoue K, Nishimaki-Mogami T: Structure-activity relationship of bile acids and bile acid analogs in regard to FXR activation. J Lipid Res. 2004 Jan;45(1):132-8. Epub 2003 Sep 16. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- S-nitrosoglutathione binding
- Specific Function
- Conjugation of reduced glutathione to a wide number of exogenous and endogenous hydrophobic electrophiles. Regulates negatively CDK5 activity via p25/p35 translocation to prevent neurodegeneration.
- Gene Name
- GSTP1
- Uniprot ID
- P09211
- Uniprot Name
- Glutathione S-transferase P
- Molecular Weight
- 23355.625 Da
References
- Nobuoka A, Takayama T, Miyanishi K, Sato T, Takanashi K, Hayashi T, Kukitsu T, Sato Y, Takahashi M, Okamoto T, Matsunaga T, Kato J, Oda M, Azuma T, Niitsu Y: Glutathione-S-transferase P1-1 protects aberrant crypt foci from apoptosis induced by deoxycholic acid. Gastroenterology. 2004 Aug;127(2):428-43. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- G-protein coupled bile acid receptor activity
- Specific Function
- Receptor for bile acid. Bile acid-binding induces its internalization, activation of extracellular signal-regulated kinase and intracellular cAMP production. May be involved in the suppression of m...
- Gene Name
- GPBAR1
- Uniprot ID
- Q8TDU6
- Uniprot Name
- G-protein coupled bile acid receptor 1
- Molecular Weight
- 35247.795 Da
References
- Yoneno K, Hisamatsu T, Shimamura K, Kamada N, Ichikawa R, Kitazume MT, Mori M, Uo M, Namikawa Y, Matsuoka K, Sato T, Koganei K, Sugita A, Kanai T, Hibi T: TGR5 signalling inhibits the production of pro-inflammatory cytokines by in vitro differentiated inflammatory and intestinal macrophages in Crohn's disease. Immunology. 2013 May;139(1):19-29. doi: 10.1111/imm.12045. [Article]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Glutathione transferase activity
- Specific Function
- Conjugation of reduced glutathione to a wide number of exogenous and endogenous hydrophobic electrophiles.
Components:
References
- Zakharyan RA, Sampayo-Reyes A, Healy SM, Tsaprailis G, Board PG, Liebler DC, Aposhian HV: Human monomethylarsonic acid (MMA(V)) reductase is a member of the glutathione-S-transferase superfamily. Chem Res Toxicol. 2001 Aug;14(8):1051-7. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- Transporter activity
- Specific Function
- Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes.
- Gene Name
- ABCB11
- Uniprot ID
- O95342
- Uniprot Name
- Bile salt export pump
- Molecular Weight
- 146405.83 Da
References
- Schuetz EG, Strom S, Yasuda K, Lecureur V, Assem M, Brimer C, Lamba J, Kim RB, Ramachandran V, Komoroski BJ, Venkataramanan R, Cai H, Sinal CJ, Gonzalez FJ, Schuetz JD: Disrupted bile acid homeostasis reveals an unexpected interaction among nuclear hormone receptors, transporters, and cytochrome P450. J Biol Chem. 2001 Oct 19;276(42):39411-8. doi: 10.1074/jbc.M106340200. Epub 2001 Aug 16. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent transport of organic anions such as sulfobromophthalein (BSP) and conjugated (taurocholate) and unconjugated (cholate) bile acids (By similarity). Selectively inhibit...
- Gene Name
- SLCO1A2
- Uniprot ID
- P46721
- Uniprot Name
- Solute carrier organic anion transporter family member 1A2
- Molecular Weight
- 74144.105 Da
References
- Kullak-Ublick GA, Hagenbuch B, Stieger B, Wolkoff AW, Meier PJ: Functional characterization of the basolateral rat liver organic anion transporting polypeptide. Hepatology. 1994 Aug;20(2):411-6. [Article]
- Hata S, Wang P, Eftychiou N, Ananthanarayanan M, Batta A, Salen G, Pang KS, Wolkoff AW: Substrate specificities of rat oatp1 and ntcp: implications for hepatic organic anion uptake. Am J Physiol Gastrointest Liver Physiol. 2003 Nov;285(5):G829-39. Epub 2003 Jul 3. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Bile acid:sodium symporter activity
- Specific Function
- Plays a critical role in the sodium-dependent reabsorption of bile acids from the lumen of the small intestine. Plays a key role in cholesterol metabolism.
- Gene Name
- SLC10A2
- Uniprot ID
- Q12908
- Uniprot Name
- Ileal sodium/bile acid cotransporter
- Molecular Weight
- 37713.405 Da
References
- Craddock AL, Love MW, Daniel RW, Kirby LC, Walters HC, Wong MH, Dawson PA: Expression and transport properties of the human ileal and renal sodium-dependent bile acid transporter. Am J Physiol. 1998 Jan;274(1 Pt 1):G157-69. [Article]
- Saeki T, Matoba K, Furukawa H, Kirifuji K, Kanamoto R, Iwami K: Characterization, cDNA cloning, and functional expression of mouse ileal sodium-dependent bile acid transporter. J Biochem. 1999 Apr;125(4):846-51. [Article]
- Saeki T, Takahashi N, Kanamoto R, Iwami K: Characterization of cloned mouse Na+/taurocholate cotransporting polypeptide by transient expression in COS-7 cells. Biosci Biotechnol Biochem. 2002 May;66(5):1116-8. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Virus receptor activity
- Specific Function
- The hepatic sodium/bile acid uptake system exhibits broad substrate specificity and transports various non-bile acid organic compounds as well. It is strictly dependent on the extracellular presenc...
- Gene Name
- SLC10A1
- Uniprot ID
- Q14973
- Uniprot Name
- Sodium/bile acid cotransporter
- Molecular Weight
- 38118.64 Da
References
- Hata S, Wang P, Eftychiou N, Ananthanarayanan M, Batta A, Salen G, Pang KS, Wolkoff AW: Substrate specificities of rat oatp1 and ntcp: implications for hepatic organic anion uptake. Am J Physiol Gastrointest Liver Physiol. 2003 Nov;285(5):G829-39. Epub 2003 Jul 3. [Article]
Drug created at June 13, 2005 13:24 / Updated at August 31, 2022 19:25