Literature DB >> 12166927

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

Roberto Pellicciari, Stefano Fiorucci, Emidio Camaioni, Carlo Clerici, Gabriele Costantino, Patrick R Maloney, Antonio Morelli, Derek J Parks, Timothy M Willson.   

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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Year:  2002        PMID： 12166927     DOI： 10.1021/jm025529g

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  189 in total

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Journal:  J Hepatol       Date:  2006-12-18       Impact factor: 25.083

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9.  FXR activation by obeticholic acid or nonsteroidal agonists induces a human-like lipoprotein cholesterol change in mice with humanized chimeric liver.

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