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459789-99-2

459789-99-2 structure
459789-99-2 structure
  • Name: Obeticholic acid
  • Chemical Name: (4R)-4-[(3R,5S,6R,7R,8S,9S,10S,13R,14S,17R)-6-ethyl-3,7-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoic acid
  • CAS Number: 459789-99-2
  • Molecular Formula: C26H44O4
  • Molecular Weight: 420.625
  • Catalog: API Digestive system medication Biliary medicine
  • Create Date: 2018-07-14 09:55:27
  • Modify Date: 2025-08-22 17:52:56
  • INT-747 is a potent and selective farnesoid X receptor (FXR) agonist with an EC50 of 99 nM.
Name (4R)-4-[(3R,5S,6R,7R,8S,9S,10S,13R,14S,17R)-6-ethyl-3,7-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoic acid
Synonyms 6α-ethyl-chenodeoxycholic acid
Cholan-24-oic acid, 6-ethyl-3,7-dihydroxy-, (3α,5β,6α,7α,8ξ)-
6alpha-Ethyl-chenodeoxycholic acid
Obeticholic acid
1osv
6-Ethylchenodeoxycholic acid
INT-747
(3α,5β,6α,7α,8ξ)-6-Ethyl-3,7-dihydroxycholan-24-oic acid
UNII-0462Z4S4OZ
6-ECDCA
OCA
CHC
Description INT-747 is a potent and selective farnesoid X receptor (FXR) agonist with an EC50 of 99 nM.
Related Catalog
Target

EC50: 99 nM (FXR)

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].
Animal Admin Initially, all animals (at 6-weeks age) are placed on a standard rodent diet for a week. Baseline blood and urine samples are collected and basal blood pressure (BP) is measured prior to grouping the animals. Subsequently, the animals are randomized into low (LS; n=9) or high salt (HS) diet groups. Hypertension is induced in the HS group by daily high-salt diet feeding and the group is subdivided to receive one of two doses of INT-747: low dose (10 mg/kg/day; n=15) or high dose (30 mg/kg/day; n=15) in 1% methylcellulose; or vehicle (1% methylcellulose in distilled water; n=15) orally everyday for 6 weeks. In parallel, the LS group also receive 1% methylcellulose. BP is measured weekly for the duration of the study as described below.
References

[1]. Fiorucci S, et al. Protective effects of 6-ethyl chenodeoxycholic acid, a farnesoid X receptor ligand, in estrogen-induced cholestasis. J Pharmacol Exp Ther. 2005 May;313(2):604-12.

[2]. Ghebremariam YT, et al. FXR agonist INT-747 upregulates DDAH expression and enhances insulin sensitivity in high-salt fed Dahl rats. PLoS One. 2013 Apr 4;8(4):e60653.

[3]. Verbeke L, et al. The FXR Agonist Obeticholic Acid Prevents Gut Barrier Dysfunction and Bacterial Translocation in Cholestatic Rats. Am J Pathol. 2015 Feb;185(2):409-19.
Density 1.1±0.1 g/cm3
Boiling Point 562.9±25.0 °C at 760 mmHg
Molecular Formula C26H44O4
Molecular Weight 420.625
Flash Point 308.3±19.7 °C
Exact Mass 420.323975
PSA 77.76000
LogP 5.68
Vapour Pressure 0.0±3.5 mmHg at 25°C
Index of Refraction 1.530
Hazard Codes Xi
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