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INT-767 CAS: 1000403-03-1

Category: Inhibitors
Product Name: INT-767
Cat No: I000064
CAS No: 1000403-03-1
Molecular Formula: C25H43NaO6S
Molecular Weight: 494.66
SMILES: O[C@@H]1CC[C@@]2(C)[C@@]([C@@H](CC)[C@@H](O)[C@]3([H])[C@]2([H])CC[C@@]4(C)[C@@]3([H])CC[C@@]4([C@H](C)CCOS(=O)([O-])=O)[H])([H])C1.[Na+]
InChI: InChI=1S/C25H44O6S.Na/c1-5-17-21-14-16(26)8-11-25(21,4)20-9-12-24(3)18(6-7-19(24)22(20)23(17)27)15(2)10-13-31-32(28,29)30;/h15-23,26-27H,5-14H2,1-4H3,(H,28,29,30);/q;+1/p-1/t15-,16-,17-,18-,19+,20+,21+,22+,23-,24-,25-;/m1./s1
InChIKey: TXIWHUPIUUZFFK-PMWRKVJASA-M
Solubility: DMSO: ≥ 205.5 mg/mL
Target: FXR/TGR5
IC50: 30 nM(EC50, FXR), 630 nM(EC50, TGR5) [2]
CAS 1000403-03-1,INT-767
  • Description

INT-767(cas 1000403-03-1) is a inhibitor of FXR and TGF5 and could have probable effect against some liver and metabolic diseases. It was just planed a Phase II trial for Hepatic fibrosis. IC50: 30 nM(EC50, FXR), 630 nM(EC50, TGR5).

  • Spec

Appearance:Solid powder
Purity: > 98%

  • References

1: Rizzo G, Passeri D, De Franco F, Ciaccioli G, Donadio L, Rizzo G, Orlandi S, Sadeghpour B, Wang XX, Jiang T, Levi M, Pruzanski M, Adorini L. Functional characterization of the semisynthetic bile acid derivative INT-767, a dual farnesoid X receptor and TGR5 agonist. Mol Pharmacol. 2010 Oct;78(4):617-30. doi: 10.1124/mol.110.064501. Epub 2010 Jul 14. PubMed PMID: 20631053; PubMed Central PMCID: PMC2981390.
2: Baghdasaryan A, Claudel T, Gumhold J, Silbert D, Adorini L, Roda A, Vecchiotti S, Gonzalez FJ, Schoonjans K, Strazzabosco M, Fickert P, Trauner M. Dual farnesoid X receptor/TGR5 agonist INT-767 reduces liver injury in the Mdr2-/- (Abcb4-/-) mouse cholangiopathy model by promoting biliary HCO⁻₃ output. Hepatology. 2011 Oct;54(4):1303-12. doi: 10.1002/hep.24537. PubMed PMID: 22006858; PubMed Central PMCID: PMC3744065.
3: Wang XX, Luo Y, Wang D, Adorini L, Pruzanski M, Dobrinskikh E, Levi M. A Dual Agonist of Farnesoid X Receptor (FXR) and the G protein-coupled Receptor TGR5, INT-767, Slows Down Age-Related Kidney Disease in Mice. J Biol Chem. 2017 Jun 8. pii: jbc.C117.794982. doi: 10.1074/jbc.C117.794982. [Epub ahead of print] PubMed PMID: 28596381.


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