Formulation: A solid
Formal Name: 1-(4'-((5-cyclopropyl-3-(2,6-dichlorophenyl)isoxazol-4-yl)methoxy)-[1,1'-biphenyl]-3-yl)cyclopropane-1-carboxylic acid
Purity: ≥90%
Formula Markup: C29H23Cl2NO4
Formula Weight: 520,4
Shelf life (days): 1095
Notes: ZLY28 is a farnesoid X receptor (FXR) agonist and an inhibitor of fatty acid binding protein 1 (FABP1).{67410} It selectively induces reporter gene expression in HepG2 cells expressing human FXR (EC50 = 143 nM) over cells expressing 19 other receptors (EC50s = >10,000 nM for all). ZLY28 selectively inhibits FABP1 (IC50 = 2.7 µM) over FABP3 (IC50 = >30 µM) but also inhibits FABP4 (IC50 = 6.3 µM). In vivo, ZLY28 (20 mg/kg) induces FXR-related gene expression in the ileum but not the liver in a mouse model of carbon tetrachloride-induced non-alcoholic steatohepatitis (NASH). It also reduces hepatocyte ballooning, as well as hepatic lobular inflammation and steatosis in the same model.