A dual FFAR1 and PPARδ agonist
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ZLY032

Item No. 31485

Technical Information
Formal Name
(3S)-2,3-dihydro-6-[[4-methyl-2-[4-(trifluoromethyl)phenyl]-5-thiazolyl]methoxy]-3-benzofuranacetic acid
CAS Number
2314465-67-1
Molecular Formula
C22H18F3NO4S
Formula Weight
Purity
≥98%
Formulation
A solid
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:5): 0.16 mg/ml
λmax
308 nm
SMILES
CC(N=C(C1=CC=C(C(F)(F)F)C=C1)S2)=C2COC3=CC=C([C@H](CC(O)=O)CO4)C4=C3
InChi Code
InChI=1S/C22H18F3NO4S/c1-12-19(31-21(26-12)13-2-4-15(5-3-13)22(23,24)25)11-29-16-6-7-17-14(8-20(27)28)10-30-18(17)9-16/h2-7,9,14H,8,10-11H2,1H3,(H,27,28)/t14-/m1/s1
InChi Key
YBBZJHLFUPKHJD-CQSZACIVSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product 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 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Li, Z., Chen, Y., Zhou, Z., et alDiscovery of first-in-class thiazole-based dual FFA1/PPARδ agonists as potential anti-diabetic agents. Eur. J. Med. Chem. 164, 352-365 (2019).

    2. Li, Z., Zhou, Z., Hu, L., et alZLY032, the first-in-class dual FFA1/PPARδ agonist, improves glucolipid metabolism and alleviates hepatic fibrosis. Pharmacol Res. 159, 105035 (2020).