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INT-747

    Detailed Description

    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].

    Target:Aurora Kinase

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