HPG1860 is a farnesoid X receptor (FXR) agonist.1 It induces luminescence in a reporter assay using HEK293T cells expressing human FXR (EC50 = 18 nM). In vivo, HPG1860 (1, 3, or 10 mg/kg per day) decreases the serum levels of alanine transaminase (ALT) and total cholesterol, as well as hepatic inflammation, fat levels, and fibrosis, in a mouse model of non-alcoholic steatohepatitis (NASH) induced by a high-fat diet and carbon tetrachloride (CCl4).
References:
[1]. Mo, C., Xu, X., Zhang, P., et al.Discovery of HPG1860, a structurally novel nonbile acid FXR agonist currently in clinical development for the treatment of nonalcoholic steatohepatitisJ. Med. Chem.66(14)9363-9375(2023).