DC Chemicals · Product datasheet

Obeticholic acid (INT-747) — Datasheet

CAT. NO. DC7430

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ParameterValue
Chemical NameObeticholic Acid
CAS No.459789-99-2
Synonyms6-Ethylchenodeoxycholic acid;6alpha-Ethyl-chenodeoxycholic acid;6-Ecdca;6-Ethyl-cdca;C15636;6-Ethylchenodeoxycholic acid(Obeticholic Acid);Obeticholic Acid;(3α,5β,6α,7α)-6-ethyl-3,7-dihydroxy-cholan-24-oic acid;(R)-4-((3R,5S,6R,7R,8S,9S,10S,13R,14S,17R)-6-ethyl-3,7-dihydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)pentanoic acid;Obeticholic acid 6-ECDCA;INT-747;1osv;CHC;INT747;UNII-0462Z4S4OZ;Obecholic acid
FormulaC26H44O4
M.Wt420.63
SMILESC[C@@]([C@]1([H])[C@@H](CC)[C@H]2O)(CC[C@@H](O)C1)[C@]3([H])[C@]2([H])[C@@](CC[C@]4([H])[C@H](C)CCC(O)=O)([H])[C@]4(C)CC3
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

INT-747 is a potent and selective farnesoid X receptor (FXR) agonist with an EC50 of 99 nM.

In Vitro

6-ECDCA increases the expression of FXR-regulated genes in rat hepatocytes[1]. INT-747 reduces expression of liver JNK-1 and JNK-2[2]. INT-747 (256 μg/mL) shows complete inhibition of bacterial growth in all strains tested. Intestinal permeability remains unaffected after INT-747-addition to an IFN-γ-exposed intestinal epithelium of Caco-2 cells[3].

In Vivo

6-ECDCA (10 mg/kg/day) completely reverted cholestasis induced by E217α. Administration of 6-ECDCA partially prevents the impairment in total bile acid output caused by E217α by increasing the relative abundance of β-MCA and TCDCA and TDCA[1]. INT-747 (10 mg/kg) and HS increases the pulmonary congestion in the animals.INT-747 does not improve renal pathology in the HS-fed animals[2]. INT-747 (5 mg/kg) significantly increases survival in BDL rats. INT-747-treated BDL rats exhibits a significant selective ileal increase in expression of pore-closing claudin-1. Ileal expression of ZO-1 is significantly up-regulated in INT-747-treated BDL rats[3].

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

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