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Overview
- Description
- A smoothing product used in a variety of cosmetic products, and a preservative added to many medications because of its ability to kill germs.
- Description
- A smoothing product used in a variety of cosmetic products, and a preservative added to many medications because of its ability to kill germs.
- DrugBank ID
- DB04398
- Type
- Small Molecule
- Clinical Trials
- Phase 0
- 2
- Phase 1
- 10
- Phase 2
- 28
- Phase 3
- 73
- Phase 4
- 39
Identification
- Summary
Lactic acid is an emollient and keratolytic used agent in various cosmetic products and used as an additive in various pharmaceutical products for its antibacterial properties.
- Brand Names
- Dextrose and Electrolyte No. 75, Dianeal, Dianeal Low Calcium 1.5, Dianeal Pd-2/1.5, Extraneal, Glycerolyte 57, Ionosol-MB, Lactate 1-2-3, Lactated Ringers, Nxstage Pureflow, Plasma-lyte R, Prismasol, Ringers
- Generic Name
- Lactic acid
- DrugBank Accession Number
- DB04398
- Background
A normal intermediate in the fermentation (oxidation, metabolism) of sugar. The concentrated form is used internally to prevent gastrointestinal fermentation. (From Stedman, 26th ed) Sodium lactate is the sodium salt of lactic acid, and has a mild saline taste. It is produced by fermentation of a sugar source, such as corn or beets, and then, by neutralizing the resulting lactic acid to create a compound having the formula NaC3H5O3.
Lactic acid was one of active ingredients in Phexxi, a non-hormonal contraceptive agent that was approved by the FDA on May 2020.1
- Type
- Small Molecule
- Groups
- Approved, Vet approved
- Structure
Structure for Lactic acid (DB04398)
- Weight
- Average: 90.0779
Monoisotopic: 90.031694058 - Chemical Formula
- C3H6O3
- Synonyms
- (±)-2-hydroxypropanoic acid
- 2-Hydroxypropanoic acid
- 2-Hydroxypropionic acid
- ácido láctico
- Acidum lacticum
- DL- lactic acid
- DL-Lactic Acid
- DL-Milchsäure
- Lactic acid
- Lacticum acidum
- Milchsäure
- Milk acid
- rac-lactic acid
- α-hydroxypropanoic acid
- α-hydroxypropionic acid
- External IDs
- BRN 5238667
- CCRIS 2951
- E270
- NSC 367919
- SY-83
Pharmacology
- Indication
For use as an alkalinizing agent.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used in combination to treat Corns Combination Product in combination with: Polidocanol (DB06811), Salicylic acid (DB00936) ••• ••• •••••••• Used in combination for therapy Dehydration Combination Product in combination with: D-glucose (DB01914), Sodium chloride (DB09153), Calcium chloride (DB01164), Zinc gluconate (DB11248), Potassium chloride (DB00761), Magnesium chloride (DB09407) ••• ••• ••••••• ••••••••• •••••••• Used in combination for therapy Fluid loss Combination Product in combination with: Potassium chloride (DB00761), Sodium hydroxide (DB11151), Calcium chloride (DB01164), Sodium chloride (DB09153) •••••••••••• •••••••••• •••••••• Used in combination to treat Hyperkeratosis Combination Product in combination with: Salicylic acid (DB00936) •••••••••••• ••••• Used in combination to treat Lichenification Combination Product in combination with: Salicylic acid (DB00936), Polidocanol (DB06811) ••• ••• •••••••• - Associated Therapies
- Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Lactic acid produces a metabolic alkalinizing effect.
- Mechanism of action
Lactate ions are metabolized ultimately to carbon dioxide and water, which requires the consumption of hydrogen cations.
Target Actions Organism UBifunctional protein PutA Not Available Escherichia coli (strain K12) UNimA-related protein Not Available Deinococcus radiodurans (strain ATCC 13939 / DSM 20539 / JCM 16871 / LMG 4051 / NBRC 15346 / NCIMB 9279 / R1 / VKM B-1422) - Absorption
Not Available
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
- Not Available
- Route of elimination
Not Available
- 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. View sample adverse effects data in our new Data Library!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.Not Available
- 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.- Product Ingredients
Ingredient UNII CAS InChI Key Sodium lactate TU7HW0W0QT 72-17-3 NGSFWBMYFKHRBD-UHFFFAOYSA-M - Active Moieties
Name Kind UNII CAS InChI Key Sodium cation ionic LYR4M0NH37 17341-25-2 FKNQFGJONOIPTF-UHFFFAOYSA-N - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Lactic Acid Lotion 1 g/10mL Topical Stratus Pharmaceuticals 2009-01-08 2017-05-03 US 
Lactic Acid Cream 100 mg/1g Topical River's Edge Pharmaceuticals, LLC 2006-06-01 2011-11-30 US Lactic Acid Cream 11.34 g/113.4g Topical Stratus Pharmaceuticals 2009-01-16 2017-05-03 US Lactic Acid Lotion .1 mL/1mL Topical River's Edge Pharmaceuticals, LLC 2006-06-01 2010-02-28 US Lactinol Lotion 35.484 mL/354.84mL Topical Pedinol Pharmacal, Inc. 1992-02-01 2009-10-26 US - Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Cheongin Haejanghwan Pellet 0.001 g/1g Oral Entechbio Co., Ltd 2011-02-18 Not applicable US Cheongin Haewoohwan Pellet 0.001 g/1g Oral Entechbio Co., Ltd 2011-02-18 Not applicable US Cheongin Samrakhwan Pellet 0.001 g/1g Oral Entechbio Co., Ltd 2011-02-17 Not applicable US Cluederm Aqua Solution Peel Plus Liquid 45 mg/500mL Topical Classys Inc. 2018-07-19 2019-03-29 US Fresh Morning Bifidus bifidus Powder 0.0316 mg/1mg Oral Saimdang Cosmetics Co., Ltd 2010-08-21 Not applicable US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image (40 Mmols/l) Potassium Chloride In Lactated Ringer's Injection USP Sodium lactate (310 mg / 100 mL) + Calcium chloride (20 mg / 100 mL) + Potassium chloride (328 mg / 100 mL) + Sodium chloride (600 mg / 100 mL) Solution Intravenous Baxter Laboratories 2002-12-11 2016-07-15 Canada 
5% Dextrose In Lactated Ringer's Injection Sodium lactate (310 mg / 100 mL) + Calcium chloride (20 mg / 100 mL) + Dextrose, unspecified form (5 g / 100 mL) + Potassium chloride (30 mg / 100 mL) + Sodium chloride (600 mg / 100 mL) Solution Intravenous B. Braun Medical Inc. 1993-12-31 2012-04-10 Canada AnubisMed Lactic acid (5 g/50mL) + Ammonia (2.75 g/50mL) + Ascorbyl glucoside (0.25 g/50mL) + Ethanol (6.3 mL/50mL) + Ethylhexylglycerin (0.025 g/50mL) + Glycolic acid (17 g/50mL) + Hexylresorcinol (1 g/50mL) + Hydroxyethyl cellulose (0.34875 g/50mL) + Isopropyl alcohol (0.75 g/50mL) + Kojic acid (2.5 g/50mL) + Phenoxyethanol (0.225 g/50mL) + Propylene glycol (0.5 g/50mL) + Salicylic acid (1 g/50mL) + Water (7.333 mL/50mL) Liquid Topical ANUBIS COSMETICS SL 2022-11-04 2027-07-01 US AZONEFROL-PD PERİTON DİYALİZ ÇÖZELTİSİ, 2000 ML ÇİFTLİ TORBA Sodium lactate (4480 mg/L) + Alanine (951 mg/L) + Arginine (1071 mg/L) + Calcium chloride dihydrate (184 mg/L) + Glycine (510 mg/L) + Histidine (714 mg/L) + Isoleucine (850 mg/L) + Leucine (1020 mg/L) + Lysine hydrochloride (955 mg/L) + Magnesium chloride hexahydrate (51 mg/L) + N-Acetylmethionine (850 mg/L) + Phenylalanine (570 mg/L) + Proline (595 mg/L) + Serine (510 mg/L) + Sodium chloride (5380 mg/L) + Threonine (646 mg/L) + Tryptophan (270 mg/L) + Tyrosine (300 mg/L) + Valine (1393 mg/L) Solution Intraperitoneal POLİFARMA İLAÇ SAN. VE TİC. A.Ş. 2019-05-23 Not applicable Turkey 
AZONEFROL-PD PERİTON DİYALİZ ÇÖZELTİSİ, 2000 ML TEKLİ TORBA Sodium lactate (4480 mg/L) + Alanine (951 mg/L) + Arginine (1071 mg/L) + Calcium chloride dihydrate (184 mg/L) + Glycine (510 mg/L) + Histidine (714 mg/L) + Isoleucine (850 mg/L) + Leucine (1020 mg/L) + Lysine hydrochloride (955 mg/L) + Magnesium chloride hexahydrate (51 mg/L) + N-Acetylmethionine (850 mg/L) + Phenylalanine (570 mg/L) + Proline (595 mg/L) + Serine (510 mg/L) + Sodium chloride (5380 mg/L) + Threonine (646 mg/L) + Tryptophan (270 mg/L) + Tyrosine (300 mg/L) + Valine (1393 mg/L) Solution Intraperitoneal POLİFARMA İLAÇ SAN. VE TİC. A.Ş. 2019-05-23 Not applicable Turkey - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image 1/6 MOLAR SODYUM LAKTAT 1000 ML SOLUSYON SETLI SISE Sodium lactate (1.87 g/100mL) Solution Intravenous OSEL İLAÇ SAN. VE TİC. A.Ş. 2018-12-25 Not applicable Turkey 1/6 MOLAR SODYUM LAKTAT 1000 ML SOLUSYON SETSIZ SISE Sodium lactate (1.87 g/100mL) Solution Intravenous OSEL İLAÇ SAN. VE TİC. A.Ş. 2018-12-25 Not applicable Turkey 1/6 MOLAR SODYUM LAKTAT 500 ML SOLUSYON SETLI SISE Sodium lactate (1.87 g/100mL) Solution Intravenous OSEL İLAÇ SAN. VE TİC. A.Ş. 2018-12-25 Not applicable Turkey 1/6 MOLAR SODYUM LAKTAT 500 ML SOLUSYON SETSIZ SISE Sodium lactate (1.87 g/100mL) Solution Intravenous OSEL İLAÇ SAN. VE TİC. A.Ş. 2018-12-25 Not applicable Turkey BALANCE %1,5 GLIKOZ 1,25 MMOL / 1 KALSIYUM 2000 ML BIOFIN TORBA Sodium lactate (3.925 g/L) + Calcium chloride dihydrate (0.1838 g/L) + D-glucose monohydrate (16.5 g/L) + Magnesium chloride hexahydrate (0.1017 g/L) + Sodium chloride (5.64 g/L) Solution Intraperitoneal FRESENIUS MEDİKAL HİZMETLER A.Ş. 2013-01-29 Not applicable Turkey
Categories
- ATC Codes
- G01AD01 — Lactic acid
- Drug Categories
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as alpha hydroxy acids and derivatives. These are organic compounds containing a carboxylic acid substituted with a hydroxyl group on the adjacent carbon.
- Kingdom
- Organic compounds
- Super Class
- Organic acids and derivatives
- Class
- Hydroxy acids and derivatives
- Sub Class
- Alpha hydroxy acids and derivatives
- Direct Parent
- Alpha hydroxy acids and derivatives
- Alternative Parents
- Secondary alcohols / Monocarboxylic acids and derivatives / Carboxylic acids / Organic oxides / Hydrocarbon derivatives / Carbonyl compounds
- Substituents
- Alcohol / Aliphatic acyclic compound / Alpha-hydroxy acid / Carbonyl group / Carboxylic acid / Carboxylic acid derivative / Hydrocarbon derivative / Monocarboxylic acid or derivatives / Organic oxide / Organic oxygen compound
- Molecular Framework
- Aliphatic acyclic compounds
- External Descriptors
- 2-hydroxy monocarboxylic acid (CHEBI:78320)
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- 3B8D35Y7S4
- CAS number
- 50-21-5
- InChI Key
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N
- InChI
- InChI=1S/C3H6O3/c1-2(4)3(5)6/h2,4H,1H3,(H,5,6)
- IUPAC Name
- 2-hydroxypropanoic acid
- SMILES
- CC(O)C(O)=O
References
- Synthesis Reference
Yoshihide Hagiwara, Miyauchi Tetsuji, Yuki Morimasa, "Process for preparing food products containing a lactic acid bacteria-fermented product of a cereal germ." U.S. Patent US4056637, issued February, 1933.
US4056637- General References
- External Links
- Human Metabolome Database
- HMDB0144295
- KEGG Drug
- D00111
- KEGG Compound
- C01432
- PubChem Compound
- 612
- PubChem Substance
- 46505582
- ChemSpider
- 592
- BindingDB
- 23233
- 1314409
- ChEBI
- 78320
- ChEMBL
- CHEMBL1200559
- Guide to Pharmacology
- GtP Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Lactic_acid
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Completed Not Available Acute Pancreatitis 1 somestatus stop reason just information to hide Not Available Completed Basic Science Perfusions 1 somestatus stop reason just information to hide Not Available Completed Basic Science Type 1 Diabetes Mellitus With Hypoglycemia 1 somestatus stop reason just information to hide Not Available Completed Diagnostic Post Cardiac Surgery 1 somestatus stop reason just information to hide Not Available Completed Other Healthy Volunteers (HV) / Hyperlactatemia / Lactate 2 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Contract Pharm
- Groupe Parima Inc.
- Paddock Labs
- PEDiNOL
- Philipp Thomas Usa LLC
- Rising Pharmaceuticals
- River's Edge Pharmaceuticals
- Sheffield Laboratories Div Faria Limited LLC
- Sonar Products Inc.
- Stratus Pharmaceuticals Inc.
- Synthera Dr Friedrichs Gmgh Co. KG
- Dosage Forms
Form Route Strength Solution Intravenous 1.87 g/100mL Gel Vaginal 225 mg Solution Intraperitoneal 0.2573 g/l Solution Intraperitoneal 0.1838 g/L Pellet Oral 0.001 g/1g Liquid Topical 45 mg/500mL Solution Intravenous 0.27 g/1000ml Solution Intraperitoneal Injection, solution Intravenous Solution Intraperitoneal; Irrigation Injection, solution Intraperitoneal Liquid Hemodialysis Solution Solution Topical Solution Topical 16.7 % Tincture Topical Solution Intraperitoneal 25.7 mg/100ml Powder Oral 0.0316 mg/1mg Solution Other 57 g/100ml Solution Unknown Solution Extracorporeal Solution Intravenous 600.0 mg Solution Hemodialysis; Intravenous Liquid Topical 0.01 mg/1mL Liquid Intraperitoneal Solution Hemodialysis; Intraperitoneal Patch Topical Tablet, chewable Oral Lotion Topical 12 g Solution Oral 160 g/L Injection Intravenous 20 mg/100ml Liquid Irrigation Irrigant Irrigation Solution, for slush Irrigation Solution Irrigation Solution Intravenous; Irrigation Cream Topical 100 mg/1g Lotion Topical .1 mL/1mL Lotion Topical 1 g/10mL Cream Topical Gel Topical Solution Topical 0.3 mg/30mL Lotion Topical Cream Topical 10 % Lotion Topical 35.484 mL/354.84mL Cream Topical 11.34 g/113.4g Injection Intravenous 0.027 % w/v Solution Intraperitoneal 0.184 g/l Solution Oral Lotion Topical 5 % Injection Intravenous Liquid Intravenous Capsule, gelatin coated Oral Solution Hemodialysis; Intravenous 0.27 g/l Kit Hemodialysis Solution Intravenous Solution Hemodialysis Solution Hemodialysis 0.257 g/l Solution Intravenous 0.1 g/500ml Solution Irrigation; Topical Solution Topical 8.85 % w/v Solution Intravenous 50.000 mL Solution Oral 11.700 mg Injection, solution Parenteral Injection, solution Parenteral 11.2 % Injection, solution, concentrate Intravenous Injection, solution Parenteral 1.87 % Injection, solution Intravenous 1.87 g/100mL Injection, solution, concentrate Intravenous 5.6 g/10mL Solution Parenteral 2.500 g Solution Oral 0.012 g Injection, solution, concentrate Intravenous Solution Parenteral Gel Vaginal 4.5 g Syrup Cutaneous Liquid Topical - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US6077836 No 2000-06-20 2017-06-20 US US6248726 No 2001-06-19 2018-06-19 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 16.8 °C PhysProp boiling point (°C) 122 °C at 1.50E+01 mm Hg PhysProp water solubility 1E+006 mg/L MERCK INDEX (1996) logP -0.72 HANSCH,C ET AL. (1995) pKa 3.86 (at 20 °C) KORTUM,G ET AL (1961) - Predicted Properties
Property Value Source Water Solubility 562.0 mg/mL ALOGPS logP -0.79 ALOGPS logP -0.47 Chemaxon logS 0.79 ALOGPS pKa (Strongest Acidic) 3.78 Chemaxon pKa (Strongest Basic) -3.7 Chemaxon Physiological Charge -1 Chemaxon Hydrogen Acceptor Count 3 Chemaxon Hydrogen Donor Count 2 Chemaxon Polar Surface Area 57.53 Å2 Chemaxon Rotatable Bond Count 1 Chemaxon Refractivity 18.84 m3·mol-1 Chemaxon Polarizability 8.05 Å3 Chemaxon Number of Rings 0 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 108.5032215 predictedDarkChem Lite v0.1.0 [M-H]- 124.62436 predictedDeepCCS 1.0 (2019) [M+H]+ 110.0780215 predictedDarkChem Lite v0.1.0 [M+H]+ 127.41325 predictedDeepCCS 1.0 (2019) [M+Na]+ 108.9897215 predictedDarkChem Lite v0.1.0 [M+Na]+ 135.60988 predictedDeepCCS 1.0 (2019)
Targets
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- Kind
- Protein
- Organism
- Escherichia coli (strain K12)
- Pharmacological action
- Unknown
- Curator comments
- The references provide evidence of inhibition by lactate molecule.
- General Function
- Oxidizes proline to glutamate for use as a carbon and nitrogen source and also function as a transcriptional repressor of the put operon.
- Specific Function
- 1-pyrroline-5-carboxylate dehydrogenase activity
- Gene Name
- putA
- Uniprot ID
- P09546
- Uniprot Name
- Bifunctional protein PutA
- Molecular Weight
- 143813.665 Da
References
- Zhang M, White TA, Schuermann JP, Baban BA, Becker DF, Tanner JJ: Structures of the Escherichia coli PutA proline dehydrogenase domain in complex with competitive inhibitors. Biochemistry. 2004 Oct 5;43(39):12539-48. doi: 10.1021/bi048737e. [Article]
- Lee YH, Nadaraia S, Gu D, Becker DF, Tanner JJ: Structure of the proline dehydrogenase domain of the multifunctional PutA flavoprotein. Nat Struct Biol. 2003 Feb;10(2):109-14. [Article]
- Kind
- Protein
- Organism
- Deinococcus radiodurans (strain ATCC 13939 / DSM 20539 / JCM 16871 / LMG 4051 / NBRC 15346 / NCIMB 9279 / R1 / VKM B-1422)
- Pharmacological action
- Unknown
- General Function
- Not Available
- Specific Function
- Not Available
- Gene Name
- Not Available
- Uniprot ID
- Q9RW27
- Uniprot Name
- NimA-related protein
- Molecular Weight
- 21890.23 Da
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Proton-coupled monocarboxylate symporter. Catalyzes the rapid transport across the plasma membrane of monocarboxylates such as L-lactate, pyruvate and ketone bodies, acetoacetate, beta-hydroxybutyrate and acetate (PubMed:32415067, PubMed:9786900). Dimerization is functionally required and both subunits work cooperatively in transporting substrate (PubMed:32415067)
- Specific Function
- identical protein binding
- Gene Name
- SLC16A7
- Uniprot ID
- O60669
- Uniprot Name
- Monocarboxylate transporter 2
- Molecular Weight
- 52199.745 Da
References
- Lin RY, Vera JC, Chaganti RS, Golde DW: Human monocarboxylate transporter 2 (MCT2) is a high affinity pyruvate transporter. J Biol Chem. 1998 Oct 30;273(44):28959-65. [Article]
- Broer S, Broer A, Schneider HP, Stegen C, Halestrap AP, Deitmer JW: Characterization of the high-affinity monocarboxylate transporter MCT2 in Xenopus laevis oocytes. Biochem J. 1999 Aug 1;341 ( Pt 3):529-35. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Mediates the Na(+)-independent transport of steroid sulfate conjugates and other specific organic anions (PubMed:10873595, PubMed:11159893, PubMed:11932330, PubMed:12724351, PubMed:14610227, PubMed:16908597, PubMed:18501590, PubMed:20507927, PubMed:22201122, PubMed:23531488, PubMed:25132355, PubMed:26383540, PubMed:27576593, PubMed:28408210, PubMed:29871943, PubMed:34628357). Responsible for the transport of estrone 3-sulfate (E1S) through the basal membrane of syncytiotrophoblast, highlighting a potential role in the placental absorption of fetal-derived sulfated steroids including the steroid hormone precursor dehydroepiandrosterone sulfate (DHEA-S) (PubMed:11932330, PubMed:12409283). Also facilitates the uptake of sulfated steroids at the basal/sinusoidal membrane of hepatocytes, therefore accounting for the major part of organic anions clearance of liver (PubMed:11159893). Mediates the intestinal uptake of sulfated steroids (PubMed:12724351, PubMed:28408210). Mediates the uptake of the neurosteroids DHEA-S and pregnenolone sulfate (PregS) into the endothelial cells of the blood-brain barrier as the first step to enter the brain (PubMed:16908597, PubMed:25132355). Also plays a role in the reuptake of neuropeptides such as substance P/TAC1 and vasoactive intestinal peptide/VIP released from retinal neurons (PubMed:25132355). May act as a heme transporter that promotes cellular iron availability via heme oxygenase/HMOX2 and independently of TFRC (PubMed:35714613). Also transports heme by-product coproporphyrin III (CPIII), and may be involved in their hepatic disposition (PubMed:26383540). Mediates the uptake of other substrates such as prostaglandins D2 (PGD2), E1 (PGE1) and E2 (PGE2), taurocholate, L-thyroxine, leukotriene C4 and thromboxane B2 (PubMed:10873595, PubMed:14610227, PubMed:19129463, PubMed:29871943, Ref.25). May contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable). 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:14610227, PubMed:19129463, PubMed:22201122). The exact transport mechanism has not been yet deciphered but most likely involves an anion exchange, coupling the cellular uptake of organic substrate with the efflux of an anionic compound (PubMed:19129463, PubMed:20507927, PubMed:26277985). Hydrogencarbonate/HCO3(-) acts as a probable counteranion that exchanges for organic anions (PubMed:19129463). Cytoplasmic glutamate may also act as counteranion in the placenta (PubMed:26277985). An inwardly directed proton gradient has also been proposed as the driving force of E1S uptake with a (H(+):E1S) stoichiometry of (1:1) (PubMed:20507927)
- Specific Function
- bile acid transmembrane transporter activity
- Gene Name
- SLCO2B1
- Uniprot ID
- O94956
- Uniprot Name
- Solute carrier organic anion transporter family member 2B1
- Molecular Weight
- 76697.93 Da
References
- Kobayashi D, Nozawa T, Imai K, Nezu J, Tsuji A, Tamai I: Involvement of human organic anion transporting polypeptide OATP-B (SLC21A9) in pH-dependent transport across intestinal apical membrane. J Pharmacol Exp Ther. 2003 Aug;306(2):703-8. Epub 2003 Apr 30. [Article]
- Nozawa T, Imai K, Nezu J, Tsuji A, Tamai I: Functional characterization of pH-sensitive organic anion transporting polypeptide OATP-B in human. J Pharmacol Exp Ther. 2004 Feb;308(2):438-45. Epub 2003 Nov 10. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Bidirectional proton-coupled monocarboxylate transporter (PubMed:12946269, PubMed:32946811, PubMed:33333023). Catalyzes the rapid transport across the plasma membrane of many monocarboxylates such as lactate, pyruvate, acetate and the ketone bodies acetoacetate and beta-hydroxybutyrate, and thus contributes to the maintenance of intracellular pH (PubMed:12946269, PubMed:33333023). The transport direction is determined by the proton motive force and the concentration gradient of the substrate monocarboxylate. MCT1 is a major lactate exporter (By similarity). Plays a role in cellular responses to a high-fat diet by modulating the cellular levels of lactate and pyruvate that contribute to the regulation of central metabolic pathways and insulin secretion, with concomitant effects on plasma insulin levels and blood glucose homeostasis (By similarity). Facilitates the protonated monocarboxylate form of succinate export, that its transient protonation upon muscle cell acidification in exercising muscle and ischemic heart (PubMed:32946811). Functions via alternate outward- and inward-open conformation states. Protonation and deprotonation of 309-Asp is essential for the conformational transition (PubMed:33333023)
- Specific Function
- carboxylic acid transmembrane transporter activity
- Gene Name
- SLC16A1
- Uniprot ID
- P53985
- Uniprot Name
- Monocarboxylate transporter 1
- Molecular Weight
- 53943.685 Da
References
- Lin RY, Vera JC, Chaganti RS, Golde DW: Human monocarboxylate transporter 2 (MCT2) is a high affinity pyruvate transporter. J Biol Chem. 1998 Oct 30;273(44):28959-65. [Article]
- Broer S, Schneider HP, Broer A, Rahman B, Hamprecht B, Deitmer JW: Characterization of the monocarboxylate transporter 1 expressed in Xenopus laevis oocytes by changes in cytosolic pH. Biochem J. 1998 Jul 1;333 ( Pt 1):167-74. [Article]
- Broer S, Rahman B, Pellegri G, Pellerin L, Martin JL, Verleysdonk S, Hamprecht B, Magistretti PJ: Comparison of lactate transport in astroglial cells and monocarboxylate transporter 1 (MCT 1) expressing Xenopus laevis oocytes. Expression of two different monocarboxylate transporters in astroglial cells and neurons. J Biol Chem. 1997 Nov 28;272(48):30096-102. [Article]
- Tamai I, Sai Y, Ono A, Kido Y, Yabuuchi H, Takanaga H, Satoh E, Ogihara T, Amano O, Izeki S, Tsuji A: Immunohistochemical and functional characterization of pH-dependent intestinal absorption of weak organic acids by the monocarboxylic acid transporter MCT1. J Pharm Pharmacol. 1999 Oct;51(10):1113-21. [Article]
- Takanaga H, Tamai I, Inaba S, Sai Y, Higashida H, Yamamoto H, Tsuji A: cDNA cloning and functional characterization of rat intestinal monocarboxylate transporter. Biochem Biophys Res Commun. 1995 Dec 5;217(1):370-7. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Sodium- and proton-independent thyroid hormones and aromatic acids transporter (PubMed:11827462, PubMed:18337592, PubMed:28754537). Mediates both uptake and efflux of 3,5,3'-triiodothyronine (T3) and 3,5,3',5'-tetraiodothyronine (T4) with high affinity, suggesting a role in the homeostasis of thyroid hormone levels (PubMed:18337592). Responsible for low affinity bidirectional transport of the aromatic amino acids, such as phenylalanine, tyrosine, tryptophan and L-3,4-dihydroxyphenylalanine (L-dopa) (PubMed:11827462, PubMed:28754537). Plays an important role in homeostasis of aromatic amino acids (By similarity)
- Specific Function
- amino acid transmembrane transporter activity
- Gene Name
- SLC16A10
- Uniprot ID
- Q8TF71
- Uniprot Name
- Monocarboxylate transporter 10
- Molecular Weight
- 55492.07 Da
References
- Kim DK, Kanai Y, Chairoungdua A, Matsuo H, Cha SH, Endou H: Expression cloning of a Na+-independent aromatic amino acid transporter with structural similarity to H+/monocarboxylate transporters. J Biol Chem. 2001 May 18;276(20):17221-8. Epub 2001 Feb 20. [Article]
- Kim DK, Kanai Y, Matsuo H, Kim JY, Chairoungdua A, Kobayashi Y, Enomoto A, Cha SH, Goya T, Endou H: The human T-type amino acid transporter-1: characterization, gene organization, and chromosomal location. Genomics. 2002 Jan;79(1):95-103. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Mediates the transport of prostaglandins (PGs, mainly PGE2, PGE1, PGE3, PGF2alpha, PGD2, PGH2) and thromboxanes (thromboxane B2) across the cell membrane (PubMed:11997326, PubMed:26692285, PubMed:8787677). PGs and thromboxanes play fundamental roles in diverse functions such as intraocular pressure, gastric acid secretion, renal salt and water transport, vascular tone, and fever (PubMed:15044627). Plays a role in the clearance of PGs from the circulation through cellular uptake, which allows cytoplasmic oxidation and PG signal termination (PubMed:8787677). PG uptake is dependent upon membrane potential and involves exchange of a monovalent anionic substrate (PGs exist physiologically as an anionic monovalent form) with a stoichiometry of 1:1 for divalent anions or of 1:2 for monovalent anions (PubMed:29204966). Uses lactate, generated by glycolysis, as a counter-substrate to mediate PGE2 influx and efflux (PubMed:11997326). Under nonglycolytic conditions, metabolites other than lactate might serve as counter-substrates (PubMed:11997326). Although the mechanism is not clear, this transporter can function in bidirectional mode (PubMed:29204966). When apically expressed in epithelial cells, it facilitates transcellular transport (also called vectorial release), extracting PG from the apical medium and facilitating transport across the cell toward the basolateral side, whereupon the PG exits the cell by simple diffusion (By similarity). In the renal collecting duct, regulates renal Na+ balance by removing PGE2 from apical medium (PGE2 EP4 receptor is likely localized to the luminal/apical membrane and stimulates Na+ resorption) and transporting it toward the basolateral membrane (where PGE2 EP1 and EP3 receptors inhibit Na+ resorption) (By similarity). Plays a role in endometrium during decidualization, increasing uptake of PGs by decidual cells (PubMed:16339169). Involved in critical events for ovulation (PubMed:27169804). Regulates extracellular PGE2 concentration for follicular development in the ovaries (By similarity). Expressed intracellularly, may contribute to vesicular uptake of newly synthesized intracellular PGs, thereby facilitating exocytotic secretion of PGs without being metabolized (By similarity). Essential core component of the major type of large-conductance anion channel, Maxi-Cl, which plays essential roles in inorganic anion transport, cell volume regulation and release of ATP and glutamate not only in physiological processes but also in pathological processes (By similarity). May contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable)
- Specific Function
- lipid transporter activity
- Gene Name
- SLCO2A1
- Uniprot ID
- Q92959
- Uniprot Name
- Solute carrier organic anion transporter family member 2A1
- Molecular Weight
- 70043.33 Da
References
- Chan BS, Endo S, Kanai N, Schuster VL: Identification of lactate as a driving force for prostanoid transport by prostaglandin transporter PGT. Am J Physiol Renal Physiol. 2002 Jun;282(6):F1097-102. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Proton-dependent transporter of monocarboxylates such as L-lactate and pyruvate (PubMed:11101640, PubMed:23935841, PubMed:31719150). Plays a predominant role in L-lactate efflux from highly glycolytic cells (By similarity)
- Specific Function
- lactate
- Gene Name
- SLC16A3
- Uniprot ID
- O15427
- Uniprot Name
- Monocarboxylate transporter 4
- Molecular Weight
- 49468.9 Da
References
- Manning Fox JE, Meredith D, Halestrap AP: Characterisation of human monocarboxylate transporter 4 substantiates its role in lactic acid efflux from skeletal muscle. J Physiol. 2000 Dec 1;529 Pt 2:285-93. [Article]
Drug created at June 13, 2005 13:24 / Updated at November 03, 2024 19:35