Obeticholic acid
FXR agonist / A novel cholic acid analog which acts as a potent and selective FXR agonist (EC50= 99 nM). Displays anticholeretic activity in a rat model of cholestasis.1 Promotes adipocyte differentiation and regulates adipose cell function.2 Normalizes insulin sensitivity in a rabbit model of metabolic syndrome.3 A potentially new therapeutic agent for management of non-alcoholic fatty liver disease4 and NASH5. Displays therapeutic benefit in patients with primary biliary cirrhosis.6 Active in vivo.
Biochemicals & reagents
459789-99-2
6-ECDCA; 6-Ethylchenodeoxycholic acid
1) Fiorucci et al. (2005), Protective effects of 6-ethyl chenodeoxycholic acid, a farnesoid X receptor ligand, in estrogen-induced cholestasis; J. Pharmacol. Exp. Ther., 313 604 2) Rizzo et al. (2006), The farnesoid X receptor promotes adipocyte differentiation and regulates adipose cell function in vivo; Mol. Pharmacol., 70 1164 3) Maneschi et al. (2013), FXR activation normalizes insulin sensitivity in visceral preadipocytes of a rabbit model of MetS; J. Endocrinol., 218 215 4) Carr and Reid (2015), FXR agonists as therapeutic agents for non-alcoholic fatty liver disease; Curr. Atheroscler. Rep, 17 500 5) Jahn et al. (2016), Non-Alcoholic Steatohepatitis: From Pathophysiology to Novel Therapies; Dig. Dis., 34 356 6) Hirschfield et al. (2015), Efficacy of obeticholic acid in patients with primary biliary cirrhosis and inadequade response to ursodeoxycholic acid; Gastroenterology, 148 751
-20°C
TARGET: Transcription factor -- PATHWAY: Transcription; Cholesterol metabolism -- DISEASE AREA: Diabetes; Liver disease