Identification | Back Directory | [Name]
AVE-8134 | [CAS]
304025-09-0 | [Synonyms]
AVE-8134 AVE8134,AVE 8134 Benzoic acid, 2-methyl-6-[[3-[(2-phenyl-4-oxazolyl)methoxy]propoxy]methyl]- | [Molecular Formula]
C22H23NO5 | [MDL Number]
MFCD28975298 | [MOL File]
304025-09-0.mol | [Molecular Weight]
381.42 |
Chemical Properties | Back Directory | [Boiling point ]
554.1±60.0 °C(Predicted) | [density ]
1.209±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [pka]
3.14±0.10(Predicted) |
Hazard Information | Back Directory | [Uses]
AVE-8134 is a potent PPARα agonist, with EC50 values of 100 and 3000 nM for human and rodent PPARα receptor, respectively. | [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]. | [IC 50]
PPARα: 100 nM (EC50, Human PPARα) | [storage]
Store at -20°C | [References]
[1] Schafer HL, et al. AVE8134, a novel potent PPARα agonist, improves lipid profile and glucose metabolism in dyslipidemic mice and type 2 diabetic rats. Acta Pharmacol Sin. 2012 Jan;33(1):82-90. DOI:10.1038/aps.2011.165 [2] Linz W, et al. The peroxisome proliferator-activated receptor-alpha (PPAR-alpha) agonist, AVE8134, attenuates the progression of heart failure and increases survival in rats. Acta Pharmacol Sin. 2009 Jul;30(7):935-46. DOI:10.1038/aps.2009.58 |
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BOC Sciences
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