gw-4064 and obeticholic-acid

gw-4064 has been researched along with obeticholic-acid* in 2 studies

Other Studies

2 other study(ies) available for gw-4064 and obeticholic-acid

ArticleYear
Discovery and Optimization of Non-bile Acid FXR Agonists as Preclinical Candidates for the Treatment of Nonalcoholic Steatohepatitis.
    Journal of medicinal chemistry, 2020, 11-12, Volume: 63, Issue:21

    Farnesoid X receptor (FXR) plays a key role in bile acid homeostasis, inflammation, fibrosis, and metabolism of lipid and glucose and becomes a promising therapeutic target for nonalcoholic steatohepatitis (NASH) or other FXR-dependent diseases. The phase III trial results of obeticholic acid demonstrate that the FXR agonists emerge as a promising intervention in patients with NASH and fibrosis, but this bile acid-derived FXR agonist brings severe pruritus and an elevated risk of cardiovascular disease for patients. Herein, we reported our efforts in the discovery of a series of non-bile acid FXR agonists, and 36 compounds were designed and synthesized based on the structure-based drug design and structural optimization strategies. Particularly, compound

    Topics: Animals; Binding Sites; Chemical and Drug Induced Liver Injury; Chenodeoxycholic Acid; Drug Design; Drug Evaluation, Preclinical; Half-Life; Humans; Liver; Male; Mice; Mice, Inbred C57BL; Molecular Docking Simulation; Non-alcoholic Fatty Liver Disease; Rats; Rats, Sprague-Dawley; Receptors, Cytoplasmic and Nuclear; Structure-Activity Relationship

2020
6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity.
    Journal of medicinal chemistry, 2002, Aug-15, Volume: 45, Issue:17

    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.

    Topics: Animals; Anticholesteremic Agents; Cell Line; Chenodeoxycholic Acid; Cholestasis; DNA-Binding Proteins; Humans; Ligands; Liver; Rats; Rats, Wistar; Receptors, Cytoplasmic and Nuclear; Structure-Activity Relationship; Transcription Factors

2002