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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)
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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