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

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          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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          Author and article information

          Journal
          J Med Chem
          Journal of medicinal chemistry
          American Chemical Society (ACS)
          0022-2623
          0022-2623
          Aug 15 2002
          : 45
          : 17
          Article
          jm025529g
          10.1021/jm025529g
          12166927
          0900a796-7d01-4e36-ab3b-0ac8dd3b3cad
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