| CAS |
No.41859-67-0 |
| 中文名称 |
苯扎贝特(10mM in DMSO,无菌） |
| 英文名称 |
Bezafibrate(10mM in DMSO，Sterile） |
| 分子式 |
C19H20ClNO4 |
| 分子量 |
361.82 |
| 溶解性 |
请根据自己的实验要求使用。 |
| 外观(性状) |
无菌溶液 |
| 储存条件 |
Stroe at -20℃，6 months. |
| 运输条件 |
冷冻运输 |
| 靶点 |
PPAR |
| 通路 |
Cell Cycle;DNA Damage/DNA Repair |
| 背景说明 |
Bezafibrate 是 PPAR 的激动剂。 |
| 生物活性 |
Bezafibrate is an agonist of PPAR， with EC50s of 50 μM， 60 μM， 20 μM for human PPARα， PPARγ and PPARδ， and 90 μM， 55 μM， 110 μM for murine PPARα， PPARγ and PPARδ， respectively; Bezafibrate is used as an hypolipidemic agent.[1-3] |
| In Vitro |
Bezafibrate 是 PPAR 的激动剂，对小鼠 PPARα、PPARγ 和 PPARδ 的 EC50 分别为 90 μM、55 μM、110 μM，对人 PPARα、PPARγ 和 PPARδ 的 EC50 分别为 50 μM、60 μM、20 μM PPARδ，分别为[1]。Bezafibrate (>200 μM) 对人视网膜微血管内皮细胞 (HRMEC) 和人视网膜色素上皮 ARPE-19 细胞显示出显著的细胞毒性。Bezafibrate (30-100 μM) 抑制肿瘤坏死因子 (TNF) α 诱导的炎症因子并调节 HRMEC 中 TNFα 诱导的核因子 (NF)-κB 反式激活。Bezafibrate 抑制 VEGF 诱导的 HRMECs 迁移，并抑制白细胞介素 (IL)-1β 诱导的 ARPE-19 细胞分泌 VEGF[2]。 |
| In Vivo |
Bezafibrate (0.5%) 显著降低 TallyHo 小鼠的血浆脂质和葡萄糖水平，并增加胰腺中的胰岛面积。Bezafibrate 还可以改善能量消耗和代谢灵活性。此外，Bezafibrate 可改善脂肪变性、改变脂质组成并增加肝脏中的线粒体质量[3]。 |
| 细胞实验 |
Cell viability is assessed using the CCK-8 kit. Hhuman retinal microvascular endothelial cells (HRMECs) or ARPE-19 cells are seeded at 5000 cells/well in medium containing 10% serum in 96-well plates. After a 24-h incubation， the medium is serum-starved with 1% FBS for 6 h， the CCK-8 reagent is added， and the absorbance of the resultant solution is measured at 450 nm by using a microplate reader at three time points， 24， 48， and 72 h after treatment with Bezafibrate (0， 10， 50， 100， 200， 500， and 1000 μM)[2]. |
| 动物实验 |
TallyHo mice are bred in our animal facility. Only male mice are used in the study， and mice receive a standard diet (SD)， which is supplemented with 0.5% (w/w) Bezafibrate for the Bezafibrate groups for 8 weeks. Animals are killed by isoflurane overdose， and dissected tissues are prepared as stated below. All data represent samples taken after 8 weeks of Bezafibrate (or SD) treatment unless otherwise stated[3]. |
| 数据来源文献 |
[1]. Willson TM， et al. The PPARs: from orphan receptors to drug discovery. J Med Chem. 2000 Feb 24;43(4):527-50.
[2]. Usui-Ouchi A， et al. The peroxisome proliferator-activated receptor pan-agonist bezafibrate suppresses microvascular inflammatory responses of retinal endothelial cells and vascular endothelial growth factor production in retinal pigmented epithelial cells. Int Immunopharmacol. 2017 Nov;52:70-76.
[3]. Franko A， et al. Bezafibrate ameliorates diabetes via reduced steatosis and improved hepatic insulin sensitivity in diabetic TallyHo mice. Mol Metab. 2017 Jan 6;6(3):256-266. |
| 规格 |
0.1ml 0.3ml 0.5ml 1ml 1.5ml |
| 单位 |
瓶 |
中文
英语
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