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AVE-8134

CAS No. : 304025-09-0

MCE 站：AVE-8134

产品活性：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。

研究领域：Cell Cycle/DNA Damage

作用靶点：PPAR

In Vitro: AVE8134 is a full PPARα dominated PPAR agonist, but not active on PPARδ. 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.

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. 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.

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