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ZLY032 Sale

目录号 : GC48272

A dual FFAR1 and PPARδ agonist

ZLY032 Chemical Structure

Cas No.:2314465-67-1

规格 价格 库存 购买数量
5 mg
¥599.00
现货
10 mg
¥1,147.00
现货
25 mg
¥2,707.00
现货
50 mg
¥5,106.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

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.

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)

Chemical Properties

Cas No. 2314465-67-1 SDF
Canonical 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
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 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 2.2252 mL 11.1259 mL 22.2519 mL
5 mM 0.445 mL 2.2252 mL 4.4504 mL
10 mM 0.2225 mL 1.1126 mL 2.2252 mL
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Research Update

ZLY032, the first-in-class dual FFA1/PPARδ agonist, improves glucolipid metabolism and alleviates hepatic fibrosis

Pharmacol Res 2020 Sep;159:105035.PMID:32562818DOI:10.1016/j.phrs.2020.105035

The free fatty acid receptor 1 (FFA1) and peroxisome proliferator-activated receptor δ (PPARδ) are considered as anti-diabetic targets based on their role in improving insulin secretion and resistance. Based on their synergetic mechanisms, we have previously identified the first-in-class dual FFA1/PPARδ agonist ZLY032. After long-term treatment, ZLY032 significantly improved glucolipid metabolism and alleviated fatty liver in ob/ob mice and methionine choline-deficient diet-fed db/db mice, mainly by regulating triglyceride metabolism, fatty acid β-oxidation, lipid synthesis, inflammation, oxidative stress and mitochondrial function. Notably, ZLY032 exhibited greater advantages on lipid metabolism, insulin sensitivity and pancreatic β-cell function than TAK-875, the most advanced candidate of FFA1 agonists. Moreover, ZLY032 prevented CCl4-induced liver fibrosis by reducing the expressions of genes involved in inflammation and fibrosis development. These results suggest that the dual FFA1/PPARδ agonists such as ZLY032 may be useful for the treatment of metabolic disorders.