INT-747INT-747(Obeticholic acid; 6-ECDCA) is a potent and selective FXR agonist(EC50=99 nM) endowed with anticholestatic activity.
IC50 value: 99 nM(EC50) [1]
Target: FXR agonist
in vitro: The exposure of rat hepatocytes to 1 microM 6-ECDCA caused a 3- to 5-fold induction of small heterodimer partner (Shp) and bile salt export pump (bsep) mRNA and 70 to 80% reduction of cholesterol 7alpha-hydroxylase (cyp7a1), oxysterol 12beta-hydroxylase (cyp8b1), and Na(+)/taurocholate cotransporting peptide (ntcp) [2].
in vivo: In vivo administration of 6-ECDCA protects against cholestasis induced by E(2)17alpha [2].
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Description: INT-777 INT-777(S-EMCA) is a novel potent and selective TGR5 agonist with remarkable in vivo activity (EC50=0.82 uM). IC50 value: 0.82 uM [1] Target: TGR5 agonist INT-777 shows a detergency power similar to CA (4), albeit with slightly lower water so...
United States
China 
![CAS No:459789-99-2 (4R)-4-[(3R,5S,6R,7R,8S,9S,10S,13R,14S,17R)-6-ethyl-3,7-dihydroxy-10,<br />13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,<br />17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoic acid](/structure/cas-459/459789-99-2.png)