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Identification
NameDeoxycholic Acid
Accession NumberDB03619  (EXPT01194, DB07690)
TypeSmall Molecule
GroupsApproved
Description

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.

Structure
Thumb
Synonyms
(3α,5β,12α)-3,12-dihydroxycholan-24-oic acid
3alpha,12alpha-Dihydroxy-5beta-cholanic acid
7α-deoxycholic acid
deoxycholate
desoxycholic acid
Desoxycholsäure
External Identifiers
  • ATX-101
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Belkyrasolution10 mgsubcutaneousKythera Biopharmaceuticals, Inc.2016-01-27Not applicableCanada
Kybellainjection, solution20 mg/2mLsubcutaneousKythera Biopharmaceuticals Inc.2015-05-18Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNII005990WHZZ
CAS number83-44-3
WeightAverage: 392.572
Monoisotopic: 392.292659768
Chemical FormulaC24H40O4
InChI KeyKXGVEGMKQFWNSR-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-[(1S,2S,5R,7R,10R,11S,14R,15R,16S)-5,16-dihydroxy-2,15-dimethyltetracyclo[8.7.0.0²,⁷.0¹¹,¹⁵]heptadecan-14-yl]pentanoic acid
SMILES
[H][C@@]12CC[[email protected]]([[email protected]](C)CCC(O)=O)[C@@]1(C)[C@@H](O)C[C@@]1([H])[C@@]2([H])CC[C@]2([H])C[[email protected]](O)CC[C@]12C
Taxonomy
DescriptionThis 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.
KingdomOrganic compounds
Super ClassLipids and lipid-like molecules
ClassSteroids and steroid derivatives
Sub ClassBile acids, alcohols and derivatives
Direct ParentDihydroxy bile acids, alcohols and derivatives
Alternative Parents
Substituents
  • Dihydroxy bile acid, alcohol, or derivatives
  • 3-alpha-hydroxysteroid
  • Hydroxysteroid
  • 12-hydroxysteroid
  • 3-hydroxysteroid
  • Cyclic alcohol
  • Secondary alcohol
  • Monocarboxylic acid or derivatives
  • Carboxylic acid
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Carbonyl group
  • Alcohol
  • Aliphatic homopolycyclic compound
Molecular FrameworkAliphatic homopolycyclic compounds
External Descriptors
Pharmacology
IndicationFor improvement in appearance of moderate to severe fullness associated with submental fat in adults.
PharmacodynamicsNot Available
Mechanism of actionAs 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.
Related Articles
AbsorptionDeoxycholic 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 distributionNot Available
Protein binding98%
Metabolism

Deoxycholic acid is not metabolized to any significant extent under normal conditions.

Route of eliminationThe 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 lifeNot Available
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9766
Blood Brain Barrier+0.9288
Caco-2 permeable+0.73
P-glycoprotein substrateSubstrate0.6648
P-glycoprotein inhibitor INon-inhibitor0.8737
P-glycoprotein inhibitor IIInhibitor0.5368
Renal organic cation transporterNon-inhibitor0.8537
CYP450 2C9 substrateNon-substrate0.7818
CYP450 2D6 substrateNon-substrate0.9115
CYP450 3A4 substrateSubstrate0.7407
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9456
CYP450 2D6 inhibitorNon-inhibitor0.9781
CYP450 2C19 inhibitorNon-inhibitor0.9707
CYP450 3A4 inhibitorNon-inhibitor0.8405
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9563
Ames testNon AMES toxic0.8794
CarcinogenicityNon-carcinogens0.9329
BiodegradationNot ready biodegradable0.992
Rat acute toxicity2.5624 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9622
hERG inhibition (predictor II)Non-inhibitor0.7246
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Solutionsubcutaneous10 mg
Injection, solutionsubcutaneous20 mg/2mL
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US7622130 No2007-12-102027-12-10Us
US7754230 No2007-12-102027-12-10Us
US8101593 No2010-03-022030-03-02Us
US8242294 No2008-05-162028-05-16Us
US8298556 No2005-08-032025-08-03Us
US8367649 No2010-03-022030-03-02Us
US8461140 No2008-02-212028-02-21Us
US8546367 No2008-02-212028-02-21Us
US8653058 No2010-03-022030-03-02Us
US8846066 No2005-02-082025-02-08Us
US8883770 No2008-02-212028-02-21Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point177 °CPhysProp
water solubility43.6 mg/L (at 20 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP3.50RODA,A ET AL. (1990)
logS-3.95ADME Research, USCD
Predicted Properties
PropertyValueSource
Water Solubility0.0173 mg/mLALOGPS
logP3.3ALOGPS
logP3.79ChemAxon
logS-4.3ALOGPS
pKa (Strongest Acidic)4.65ChemAxon
pKa (Strongest Basic)-0.35ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area77.76 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity109.2 m3·mol-1ChemAxon
Polarizability46.17 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
LC-MS/MSLC-MS/MS Spectrum - Quattro_QQQ 10V, Negative (Annotated)splash10-0006-0009000000-8b9c4803e9cb1d194c2eView in MoNA
LC-MS/MSLC-MS/MS Spectrum - Quattro_QQQ 25V, Negative (Annotated)splash10-0006-0009000000-cccabd9d13ac783b6e31View in MoNA
LC-MS/MSLC-MS/MS Spectrum - Quattro_QQQ 40V, Negative (Annotated)splash10-0007-2009000000-d7c20760d2074c07af22View in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QTOF (UPLC Q-Tof Premier, Waters) , Negativesplash10-0006-0009000000-269a5d1ed75b71c78ecbView in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QTOF (UPLC Q-Tof Premier, Waters) 30V, Negativesplash10-0007-0009000000-72f1acf9f31f344daaa1View in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-ITTOF (LCMS-IT-TOF) , Negativesplash10-000x-0008000900-ebb0e6a61bd8f06a21f7View in MoNA
1D NMR1H NMR SpectrumNot Available
2D NMR[1H,13C] 2D NMR SpectrumNot Available
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
  1. 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. [PubMed:25724831 ]
  2. 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. [PubMed:25684122 ]
External Links
ATC CodesNot Available
AHFS Codes
  • 92:92
PDB Entries
FDA labelDownload (3.18 MB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AbciximabThe risk or severity of adverse effects can be increased when Abciximab is combined with Deoxycholic Acid.
AcenocoumarolThe risk or severity of adverse effects can be increased when Acenocoumarol is combined with Deoxycholic Acid.
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Deoxycholic Acid.
AnagrelideThe risk or severity of adverse effects can be increased when Anagrelide is combined with Deoxycholic Acid.
ApixabanThe risk or severity of adverse effects can be increased when Apixaban is combined with Deoxycholic Acid.
ArgatrobanThe risk or severity of adverse effects can be increased when Argatroban is combined with Deoxycholic Acid.
BivalirudinThe risk or severity of adverse effects can be increased when Bivalirudin is combined with Deoxycholic Acid.
CangrelorThe risk or severity of adverse effects can be increased when Cangrelor is combined with Deoxycholic Acid.
CilostazolThe risk or severity of adverse effects can be increased when Cilostazol is combined with Deoxycholic Acid.
CitalopramThe risk or severity of adverse effects can be increased when Citalopram is combined with Deoxycholic Acid.
Citric AcidThe risk or severity of adverse effects can be increased when Citric Acid is combined with Deoxycholic Acid.
ClopidogrelThe risk or severity of adverse effects can be increased when Clopidogrel is combined with Deoxycholic Acid.
Dabigatran etexilateThe risk or severity of adverse effects can be increased when Dabigatran etexilate is combined with Deoxycholic Acid.
DalteparinThe risk or severity of adverse effects can be increased when Dalteparin is combined with Deoxycholic Acid.
DanaparoidThe risk or severity of adverse effects can be increased when Danaparoid is combined with Deoxycholic Acid.
DesirudinThe risk or severity of adverse effects can be increased when Desirudin is combined with Deoxycholic Acid.
DesvenlafaxineThe risk or severity of adverse effects can be increased when Desvenlafaxine is combined with Deoxycholic Acid.
DiclofenacThe risk or severity of adverse effects can be increased when Diclofenac is combined with Deoxycholic Acid.
DicoumarolThe risk or severity of adverse effects can be increased when Dicoumarol is combined with Deoxycholic Acid.
DiflunisalThe risk or severity of adverse effects can be increased when Diflunisal is combined with Deoxycholic Acid.
DipyridamoleThe risk or severity of adverse effects can be increased when Dipyridamole is combined with Deoxycholic Acid.
DuloxetineThe risk or severity of adverse effects can be increased when Duloxetine is combined with Deoxycholic Acid.
Edetic AcidThe risk or severity of adverse effects can be increased when Edetic Acid is combined with Deoxycholic Acid.
EdoxabanThe risk or severity of adverse effects can be increased when Edoxaban is combined with Deoxycholic Acid.
EnoxaparinThe risk or severity of adverse effects can be increased when Enoxaparin is combined with Deoxycholic Acid.
EptifibatideThe risk or severity of adverse effects can be increased when Eptifibatide is combined with Deoxycholic Acid.
EscitalopramThe risk or severity of adverse effects can be increased when Escitalopram is combined with Deoxycholic Acid.
Ethyl biscoumacetateThe risk or severity of adverse effects can be increased when Ethyl biscoumacetate is combined with Deoxycholic Acid.
EtodolacThe risk or severity of adverse effects can be increased when Etodolac is combined with Deoxycholic Acid.
FenoprofenThe risk or severity of adverse effects can be increased when Fenoprofen is combined with Deoxycholic Acid.
FloctafenineThe risk or severity of adverse effects can be increased when Floctafenine is combined with Deoxycholic Acid.
FluoxetineThe risk or severity of adverse effects can be increased when Fluoxetine is combined with Deoxycholic Acid.
FlurbiprofenThe risk or severity of adverse effects can be increased when Flurbiprofen is combined with Deoxycholic Acid.
FluvoxamineThe risk or severity of adverse effects can be increased when Fluvoxamine is combined with Deoxycholic Acid.
Fondaparinux sodiumThe risk or severity of adverse effects can be increased when Fondaparinux sodium is combined with Deoxycholic Acid.
HeparinThe risk or severity of adverse effects can be increased when Heparin is combined with Deoxycholic Acid.
IbuprofenThe risk or severity of adverse effects can be increased when Ibuprofen is combined with Deoxycholic Acid.
IndomethacinThe risk or severity of adverse effects can be increased when Indomethacin is combined with Deoxycholic Acid.
KetoprofenThe risk or severity of adverse effects can be increased when Ketoprofen is combined with Deoxycholic Acid.
KetorolacThe risk or severity of adverse effects can be increased when Ketorolac is combined with Deoxycholic Acid.
LevomilnacipranThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Deoxycholic Acid.
Mefenamic acidThe risk or severity of adverse effects can be increased when Mefenamic acid is combined with Deoxycholic Acid.
MeloxicamThe risk or severity of adverse effects can be increased when Meloxicam is combined with Deoxycholic Acid.
MilnacipranThe risk or severity of adverse effects can be increased when Milnacipran is combined with Deoxycholic Acid.
NabumetoneThe risk or severity of adverse effects can be increased when Nabumetone is combined with Deoxycholic Acid.
NadroparinThe risk or severity of adverse effects can be increased when Nadroparin is combined with Deoxycholic Acid.
NaproxenThe risk or severity of adverse effects can be increased when Naproxen is combined with Deoxycholic Acid.
OxaprozinThe risk or severity of adverse effects can be increased when Oxaprozin is combined with Deoxycholic Acid.
ParoxetineThe risk or severity of adverse effects can be increased when Paroxetine is combined with Deoxycholic Acid.
PhenindioneThe risk or severity of adverse effects can be increased when Phenindione is combined with Deoxycholic Acid.
PhenprocoumonThe risk or severity of adverse effects can be increased when Phenprocoumon is combined with Deoxycholic Acid.
PiroxicamThe risk or severity of adverse effects can be increased when Piroxicam is combined with Deoxycholic Acid.
PrasugrelThe risk or severity of adverse effects can be increased when Prasugrel is combined with Deoxycholic Acid.
RivaroxabanThe risk or severity of adverse effects can be increased when Rivaroxaban is combined with Deoxycholic Acid.
SertralineThe risk or severity of adverse effects can be increased when Sertraline is combined with Deoxycholic Acid.
SulindacThe risk or severity of adverse effects can be increased when Sulindac is combined with Deoxycholic Acid.
SulodexideThe risk or severity of adverse effects can be increased when Sulodexide is combined with Deoxycholic Acid.
Tiaprofenic acidThe risk or severity of adverse effects can be increased when Tiaprofenic acid is combined with Deoxycholic Acid.
TicagrelorThe risk or severity of adverse effects can be increased when Ticagrelor is combined with Deoxycholic Acid.
TiclopidineThe risk or severity of adverse effects can be increased when Ticlopidine is combined with Deoxycholic Acid.
TinzaparinThe risk or severity of adverse effects can be increased when Tinzaparin is combined with Deoxycholic Acid.
TirofibanThe risk or severity of adverse effects can be increased when Tirofiban is combined with Deoxycholic Acid.
TolmetinThe risk or severity of adverse effects can be increased when Tolmetin is combined with Deoxycholic Acid.
TreprostinilThe risk or severity of adverse effects can be increased when Treprostinil is combined with Deoxycholic Acid.
VenlafaxineThe risk or severity of adverse effects can be increased when Venlafaxine is combined with Deoxycholic Acid.
VilazodoneThe risk or severity of adverse effects can be increased when Vilazodone is combined with Deoxycholic Acid.
VorapaxarThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Deoxycholic Acid.
VortioxetineThe risk or severity of adverse effects can be increased when Vortioxetine is combined with Deoxycholic Acid.
WarfarinThe risk or severity of adverse effects can be increased when Warfarin is combined with Deoxycholic Acid.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Pseudomonas putida
Pharmacological action
unknown
General Function:
Steroid delta-isomerase activity
Specific Function:
Not Available
Gene Name:
ksi
Uniprot ID:
P07445
Molecular Weight:
14535.48 Da
References
  1. 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. [PubMed:10592235 ]
Kind
Protein
Organism
Geobacter sulfurreducens
Pharmacological action
unknown
General Function:
Metal ion binding
Specific Function:
Not Available
Gene Name:
ppcA
Uniprot ID:
Q8GGK7
Molecular Weight:
9747.54 Da
References
  1. 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. [PubMed:10592235 ]
Kind
Protein
Organism
Human
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 cytoplasm, thereby activating ribosomes for translation competence by allowing 80S ribosome assembly and facilitating EIF6 recycling to the nucleus, where it is required for 60S rRNA processing and nuclear...
Gene Name:
EFTUD1
Uniprot ID:
Q7Z2Z2
Molecular Weight:
125428.745 Da
References
  1. 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. [PubMed:10592235 ]
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
Molecular Weight:
37185.0 Da
References
  1. 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. [PubMed:10592235 ]
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
Molecular Weight:
52272.37 Da
References
  1. 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. [PubMed:10592235 ]
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), acts downstream of BamA, the receptor for CDI. Its role in CDI is independent of the AcrA-AcrB-TolC efflux pump complex.
Gene Name:
acrB
Uniprot ID:
P31224
Molecular Weight:
113572.75 Da
References
  1. 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. [PubMed:10592235 ]
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 subunit of the enzyme. Electrons originating in cytochrome c are transferred via the copper A center of subunit 2 and heme a of subunit 1 to the bimetallic center formed by heme a3 and copper B. This cy...
Gene Name:
ctaD
Uniprot ID:
P33517
Molecular Weight:
63146.395 Da
References
  1. 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. [PubMed:10592235 ]
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
Molecular Weight:
32930.42 Da
References
  1. 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. [PubMed:10592235 ]

Transporters

Kind
Protein
Organism
Human
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
Molecular Weight:
146405.83 Da
References
  1. 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. Epub 2001 Aug 16. [PubMed:11509573 ]
Kind
Protein
Organism
Human
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 inhibited by the grapefruit juice component naringin.
Gene Name:
SLCO1A2
Uniprot ID:
P46721
Molecular Weight:
74144.105 Da
References
  1. 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. [PubMed:8045503 ]
  2. 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. [PubMed:12842829 ]
Kind
Protein
Organism
Human
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
Molecular Weight:
37713.405 Da
References
  1. 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. [PubMed:9458785 ]
  2. 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. [PubMed:10101301 ]
  3. 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. [PubMed:12092825 ]
Kind
Protein
Organism
Human
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 presence of sodium.(Microbial infection) Acts as a receptor for hepatitis B virus.
Gene Name:
SLC10A1
Uniprot ID:
Q14973
Molecular Weight:
38118.64 Da
References
  1. 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. [PubMed:12842829 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on July 28, 2016 01:52