| Identification | Back Directory | [Name]
3-Benzofuranacetic acid, 2,3-dihydro-6-[[4-methyl-2-[4-(trifluoromethyl)phenyl]-5-thiazolyl]methoxy]-, (3S)- | [CAS]
2314465-67-1 | [Synonyms]
ZLY032
3-Benzofuranacetic acid, 2,3-dihydro-6-[[4-methyl-2-[4-(trifluoromethyl)phenyl]-5-thiazolyl]methoxy]-, (3S)- | [Molecular Formula]
C22H18F3NO4S | [MOL File]
2314465-67-1.mol | [Molecular Weight]
449.44 |
| Hazard Information | Back Directory | [Biological Activity]
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).1 It 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 the ob/ob mouse model of metabolic disease.2 It 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. | [References]
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)
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