Obeticholic acid (459789-99-2) is 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.
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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