General Information of Drug (ID: DM2LZ8F)

Drug Name
Taurocholic Acid Drug Info
Synonyms
Taurocholic acid; TAUROCHOLIC ACID; Taurocholate; Cholyltaurine; Cholaic acid; N-Choloyltaurine; Cholic acid taurine conjugate; 81-24-3; Taurine, N-choloyl-; Acidum cholatauricum; Taurine Cholate; UNII-5E090O0G3Z; HSDB 832; C26H45NO7S; 3alpha,7alpha,12alpha-Trihydroxy-5beta-cholanic acid 24-taurine; NSC25505; EINECS 201-336-2; NSC 25505; Ethanesulfonic acid, 2-(((3alpha,5beta,7alpha,12alpha)-3,7,12-trihydroxy-24-oxocholan-24-yl)amino)-; 2-((3-alpha,7-alpha,12-alpha-Trihydroxy-24-oxo-5-be ta-cholan-24-yl)amino)ethanesulfonic acid; [3H]taurocholic acid
Indication
Disease Entry ICD 11 Status REF
Type-2 diabetes 5A11 Phase 1/2 [1]
Cross-matching ID
PubChem CID
6675
ChEBI ID
CHEBI:28865
CAS Number
CAS 81-24-3
TTD Drug ID
DM2LZ8F
VARIDT Drug ID
DR01121

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Bile-salt-activated lipase (CEL) TTTRNQW CEL_HUMAN Inhibitor [2]
Ileal sodium/bile acid cotransporter (SLC10A2) TTPI1M5 NTCP2_HUMAN Modulator [3]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
Organic solute transporter subunit alpha (SLC51A) DTMEQ32 OSTA_HUMAN Terminated [4]
Apical sodium-dependent bile acid transporter (SLC10A2) DT7JELC NTCP2_HUMAN Terminated [5]
Organic solute transporter subunit beta (SLC51B) DT1V9AJ OSTB_HUMAN Terminated [4]
Organic anion transporting polypeptide 4A1 (SLCO4A1) DT8H2IC SO4A1_HUMAN Terminated [6]
Bile salt export pump (ABCB11) DTJ0EW4 ABCBB_HUMAN Terminated [7]
Sodium/taurocholate cotransporting polypeptide (SLC10A1) DT56EKP NTCP_HUMAN Terminated [8]
Multidrug resistance-associated protein 3 (ABCC3) DTQ3ZHF MRP3_HUMAN Terminated [9]
Multidrug resistance-associated protein 4 (ABCC4) DTCSGPB MRP4_HUMAN Terminated [10]
Organic anion transporting polypeptide 2B1 (SLCO2B1) DTPFTEQ SO2B1_HUMAN Terminated [11]
Organic anion transporting polypeptide 1A2 (SLCO1A2) DTE2B1D SO1A2_HUMAN Terminated [12]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Terminated [13]
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_HUMAN Terminated [14]
Organic anion transporting polypeptide 1B3 (SLCO1B3) DT9C1TS SO1B3_HUMAN Terminated [15]

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Ileal sodium/bile acid cotransporter (SLC10A2) DTT SLC10A2 5.752 5.641 5.904 6.506
Multidrug resistance-associated protein 3 (ABCC3) DTP MRP3 7.688 7.801 5.548 6.957
Organic anion transporting polypeptide 2B1 (SLCO2B1) DTP OATP2B1 8.165 6.597 6.591 6.397
Bile salt export pump (ABCB11) DTP BSEP 6.055 5.066 4.456 4.797
Breast cancer resistance protein (ABCG2) DTP BCRP 6.732 7.513 6.326 9.277
Organic anion transporting polypeptide 1A2 (SLCO1A2) DTP OATP1A2 4.365 4.466 3.248 2.632
Multidrug resistance-associated protein 4 (ABCC4) DTP MRP4 4.797 7.054 6.875 5.42
Organic anion transporting polypeptide 1B3 (SLCO1B3) DTP OATP1B3 8.873 2.17 2.485 3.322
Organic anion transporting polypeptide 4A1 (SLCO4A1) DTP OATP4A1 4.322 5.81 7.465 4.711
Apical sodium-dependent bile acid transporter (SLC10A2) DTP ASBT 5.752 5.641 5.904 6.506
Sodium/taurocholate cotransporting polypeptide (SLC10A1) DTP NTCP 10.34 6.714 6.815 6.055
Organic anion transporting polypeptide 1B1 (SLCO1B1) DTP OATP1B1 9.79 0.485 3.511 2.07
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease Type-2 diabetes
ICD Disease Classification 5A11
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Ileal sodium/bile acid cotransporter (SLC10A2) DTT SLC10A2 2.54E-01 -0.06 -0.17
Multidrug resistance-associated protein 3 (ABCC3) DTP MRP3 9.87E-01 -1.86E-01 -4.71E-01
Organic anion transporting polypeptide 2B1 (SLCO2B1) DTP OATP2B1 4.61E-01 -7.46E-02 -2.18E-01
Organic solute transporter subunit alpha (SLC51A) DTP OSTalpha 1.79E-01 -1.10E-01 -2.53E-01
Bile salt export pump (ABCB11) DTP BSEP 5.33E-01 -8.86E-02 -2.56E-01
Breast cancer resistance protein (ABCG2) DTP BCRP 1.85E-01 -1.34E-01 -4.20E-01
Organic anion transporting polypeptide 1A2 (SLCO1A2) DTP OATP1A2 1.39E-01 -6.13E-01 -6.63E-01
Multidrug resistance-associated protein 4 (ABCC4) DTP MRP4 6.77E-01 3.03E-02 1.51E-01
Organic anion transporting polypeptide 1B3 (SLCO1B3) DTP OATP1B3 5.85E-01 1.81E-01 6.68E-01
Organic anion transporting polypeptide 4A1 (SLCO4A1) DTP OATP4A1 5.51E-01 -6.63E-03 -5.81E-02
Apical sodium-dependent bile acid transporter (SLC10A2) DTP ASBT 2.54E-01 -6.48E-02 -1.69E-01
Sodium/taurocholate cotransporting polypeptide (SLC10A1) DTP NTCP 2.93E-01 2.87E-02 1.38E-01
Organic anion transporting polypeptide 1B1 (SLCO1B1) DTP OATP1B1 2.81E-01 3.67E-02 2.82E-01
Organic solute transporter subunit beta (SLC51B) DTP OSTbeta 4.32E-01 1.33E-01 1.00E+00
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4547).
2 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
3 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.
4 Functional complementation between a novel mammalian polygenic transport complex and an evolutionarily ancient organic solute transporter, OSTalpha-OSTbeta. J Biol Chem. 2003 Jul 25;278(30):27473-82.
5 Identification of a region of the ileal-type sodium/bile acid cotransporter interacting with a competitive bile acid transport inhibitor. Biochemistry. 2002 Dec 17;41(50):14916-24.
6 Identification of thyroid hormone transporters in humans: different molecules are involved in a tissue-specific manner. Endocrinology. 2001 May;142(5):2005-12.
7 Inhibition of transport across the hepatocyte canalicular membrane by the antibiotic fusidate. Biochem Pharmacol. 2002 Jul 1;64(1):151-8.
8 Modulation by drugs of human hepatic sodium-dependent bile acid transporter (sodium taurocholate cotransporting polypeptide) activity. J Pharmacol Exp Ther. 1999 Dec;291(3):1204-9.
9 Characterization of the role of polar amino acid residues within predicted transmembrane helix 17 in determining the substrate specificity of multidrug resistance protein 3. Biochemistry. 2003 Aug 26;42(33):9989-10000.
10 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
11 Functional characterization of pH-sensitive organic anion transporting polypeptide OATP-B in human. J Pharmacol Exp Ther. 2004 Feb;308(2):438-45.
12 Identification of multiple binding sites for substrate transport in bovine organic anion transporting polypeptide 1a2. Drug Metab Dispos. 2013 Mar;41(3):602-7.
13 Characterization of the role of ABCG2 as a bile acid transporter in liver and placenta. Mol Pharmacol. 2012 Feb;81(2):273-83.
14 Identification of a novel gene family encoding human liver-specific organic anion transporter LST-1. J Biol Chem. 1999 Jun 11;274(24):17159-63.
15 Effect of pregnane X receptor ligands on transport mediated by human OATP1B1 and OATP1B3. Eur J Pharmacol. 2008 Apr 14;584(1):57-65.