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2314465-67-1

2314465-67-1 Structure

2314465-67-1 Structure
IdentificationBack 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
Chemical PropertiesBack Directory
[Boiling point ]

595.8±60.0 °C(Predicted)
[density ]

1.386±0.06 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:5): 0.16 mg/ml
[form ]

A solid
[pka]

4.36±0.10(Predicted)
Hazard InformationBack Directory
[Uses]

ZLY032 is a dual FFA1/PPARδ agonist with the activity of improving glucose and lipid metabolism, alleviating liver fibrosis, and potentially inhibiting metabolic disorders.
[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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