6α-ethyl-chenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity

R Pellicciari, S Fiorucci, E Camaioni… - Journal of medicinal …, 2002 - ACS Publications
R Pellicciari, S Fiorucci, E Camaioni, C Clerici, G Costantino, PR Maloney, A Morelli…
Journal of medicinal chemistry, 2002ACS Publications
A series of 6α-alkyl-substituted analogues of chenodeoxycholic acid (CDCA) were
synthesized and evaluated as potential farnesoid X receptor (FXR) ligands. Among them, 6α-
ethyl-chenodeoxycholic acid (6-ECDCA) was shown to be a very potent and selective FXR
agonist (EC50= 99 nM) and to be endowed with anticholeretic activity in an in vivo rat model
of cholestasis.
A series of 6α-alkyl-substituted analogues of chenodeoxycholic acid (CDCA) were synthesized and evaluated as potential farnesoid X receptor (FXR) ligands. Among them, 6α-ethyl-chenodeoxycholic acid (6-ECDCA) was shown to be a very potent and selective FXR agonist (EC50 = 99 nM) and to be endowed with anticholeretic activity in an in vivo rat model of cholestasis.
ACS Publications