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CAS No. : 41859-67-0
MCE 国际站:Bezafibrate
产品活性:Bezafibrate 是 PPAR 的激动剂,对人和鼠 PPARα,PPARγ 和 PPARδ 的 EC50 分别为 50 μM,60 μM,20 μM 和 90 μM,55 μM,110 μM;Bezafibrate 是一种降血脂剂。
研究领域:Cell Cycle/DNA Damage | Vitamin D Related/Nuclear Receptor
作用靶点:PPAR
In Vitro: Bezafibrate is an agonist of PPAR, with EC50s of 90 μM, 55 μM, 110 μM for murine PPARα, PPARγ and PPARδ, and 50 μM, 60 μM, 20 μM for human PPARα, PPARγ and PPARδ, respectively. Bezafibrate (> 200 μM) shows significant cytotoxicity against human retinal microvascular endothelial cells (HRMECs) and human retinal pigment epithelial ARPE-19 cells. Bezafibrate (30-100 μM) suppresses tumor necrosis factor (TNF)α induced inflammatory factors and regulates TNFα induced nuclear factor (NF)-κB transactivation in HRMEC. Bezafibrate inhibits VEGF-induced HRMECs migration, and inhibits interleukin (IL)-1β-induced VEGF secretion of ARPE-19 cells.
In Vivo: Bezafibrate (0.5%) markedly reduces plasma lipid and glucose levels, and increases islet area in the pancreas in TallyHo mice. Bezafibrate also improves energy expenditure and metabolic flexibility. Moreover, Bezafibrate ameliorates steatosis, modifies lipid composition and increases mitochondrial mass in the liver.
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