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

  • J Med Chem. 2002 Aug 15;45(17):3569-72. doi: 10.1021/jm025529g.
Roberto Pellicciari ,  Stefano Fiorucci ,  Emidio Camaioni ,  Carlo Clerici ,  Gabriele Costantino ,  Patrick R Maloney ,  Antonio Morelli ,  Derek J Parks ,  Timothy M Willson
PMID: 12166927 DOI: 10.1021/jm025529g
Abstract

A series of 6alpha-alkyl-substituted analogues of chenodeoxycholic acid (CDCA) were synthesized and evaluated as potential farnesoid X receptor (FXR) ligands. Among them, 6alpha-ethyl-chenodeoxycholic acid (6-ECDCA) was shown to be a very potent and selective FXR Agonist (EC(50) = 99 nM) and to be endowed with anticholeretic activity in an in vivo rat model of cholestasis.

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