ZLY032

Description: ZLY032 is a dual agonist of free fatty acid receptor 1 (FFAR1/GPR40, EC50= 68 nM in a FLIPR assay) and peroxisome proliferator-activated receptor delta (PPARdelta, EC50= 102 nM in a reporter assay).1It is selective for FFAR1 and PPARdelta over PPARalpha and PPARgamma (EC50s = >10 µM for both). ZLY032 (40 mg/kg, twice per day) reduces blood glucose levels in an oral glucose tolerance test and decreases plasma total cholesterol and triglyceride levels in theob/obmouse model of metabolic disease.2It reduces hepatic steatosis and plasma alanine transaminase (ALT) and aspartate aminotransferase (AST) levels in a mouse model of non-alcoholic steatohepatitis (NASH) induced by a methionine and choline-deficient diet at the same dose. Target: Others. Smiles: C(C(O)=O)[C@H]1C=2C(=CC(OCC=3SC(=NC3C)C4=CC=C(C(F)(F)F)C=C4)=CC2)OC1. References: Li, Z., Chen, Y., Zhou, Z., et al.Discovery of first-in-class thiazole-based dual FFA1/PPARdelta agonists as potential anti-diabetic agentsEur. J. Med. Chem.164352-365(2019)