A dual FFAR1 and PPARδ agonist
货号:ajcx23760
CAS:2314465-67-1
分子式:C22H18F3NO4S
分子量：449.4
溶解度:DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:5): 0.16 mg/ml
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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 δ (PPARδ; EC₅₀= 102 nM in a reporter assay).¹It is selective for FFAR1 and PPARδ over PPARα and PPARγ (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.

1.Li, Z., Chen, Y., Zhou, Z., et al.Discovery of first-in-class thiazole-based dual FFA1/PPARδ agonists as potential anti-diabetic agentsEur. J. Med. Chem.164352-365(2019) 2.Li, Z., Zhou, Z., Hu, L., et al.ZLY032, the first-in-class dual FFA1/PPARδ agonist, improves glucolipid metabolism and alleviates hepatic fibrosisPharmacol Res.159105035(2020)