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.

References/Citations:

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 inadequate response to ursodeoxycholic acid; Gastroenterology, 148 751