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AVE-8134
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AVE-8134图片
CAS NO:304025-09-0
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
AVE-8134 是PPARα的有效激动剂,对人体和啮齿类动物的 PPARα 的EC50值分别为 100 和 3000 nM。
生物活性

AVE-8134 is a potentPPARαagonist, withEC50values of 100 and 3000 nM for human and rodentPPARαreceptor, respectively.

IC50& Target

PPARα

100 nM (EC50, Human PPARα)

体外研究
(In Vitro)

AVE8134 is a full PPARα dominated PPAR agonist, but not active on PPARδ[1]. In HUVEC, AVE8134 (1 μM) increases Ser-1177-eNOS phosphorylation but not eNOS expression. In monocytes, AVE8134 (10 μM) increases the expression of CD36 and the macrophage scavenger receptor 1, resulting in enhanced uptake of oxidized LDL[2].

体内研究
(In Vivo)

In female hApo A1 mice, AVE8134 (130 mg/kg/d, po for 12 d) dose-dependently loweres the plasma triglycerides, and increases the serum HDL-cholesterol, hApo A1 and mouse Apo E levels. In female ZDF rats, AVE8134 (3-30 mg/kg/d for 2 weeks) improves insulin-sensitivity index. In pre-diabetic male ZDF rats, AVE8134 (10 mg/kg/d for 8 weeks) produces an anti-diabetic action comparable to rosiglitazone, without the PPARγ mediated adverse effects on body weight and heart weight. In male ZDF rats, AVE8134 (20 mg/kg/d for 12 weeks) increases mRNA levels of the target genes LPL and PDK4 about 20 fold in the liver, and there is no relevant effect with rosiglitazone[1]. In post-MI rats, AVE8134 (3 mg/kg and 10 mg/kg) dose-dependently improves cardiac output, myocardial contractility and relaxation and reduces lung and left ventricular weight and fibrosis. Treatment at AVE8134 decreases plasma proBNP and arginine and increases plasma citrulline and urinary NOx/creatinine ratio. In DOCA rats, AVE8134 (3 mg/kg/d) prevents development of high blood pressure, myocardial hypertrophy and cardiac fibrosis, and ameliorates endothelial dysfunction. In old SHR, treatment with a low dose of AVE8134 (0.3 mg/kg/d) improves cardiac and vascular function and increases life expectancy without lowering blood pressure. AVE8134 reduces phenylephrine-induced hypertrophy in adult rat cardiomyocytes[2].

分子量

381.42

Formula

C22H23NO5

CAS 号

304025-09-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.