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/ Bezafibrate

苯扎贝特 /Bezafibrate {[allProObj[0].p_purity_real_show]}

货号：A137782 同义名： BM15075;Benzofibrate

Bezafibrate is the agonist of PPAR and the EC50 for PPAR⍺, PPARβ, PPARẟ is 50 , 20, and 60 nM respectively. It has hypolipidemic effect.

Bezafibrate 化学结构 CAS号：41859-67-0
Bezafibrate 化学结构
CAS号：41859-67-0
Bezafibrate 3D分子结构
CAS号：41859-67-0
Bezafibrate 化学结构 CAS号：41859-67-0
Bezafibrate 3D分子结构 CAS号：41859-67-0
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Bezafibrate 纯度/质量文件 产品仅供科研

货号：A137782 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 PPARα ↓ PPARβ/δ ↓ PPARγ ↓ PPARδ ↓ 其他靶点 纯度
Fenofibric acid ✔ 98%
GW6471 ++

PPARα, IC50: 0.24 μM

 		99%+
GSK3787 ++

PPARδ, pIC50: 6.6

 		++

PPARδ, pIC50: 6.6

 		99%+
FH535 ✔ 98%+
GW9662 +++

PPARα, IC50: 32 nM

 		+++

PPARγ, IC50: 3.3 nM

 		98%
T0070907 ++++

PPARγ, IC50: 1 nM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Bezafibrate 生物活性

描述 Bezafibrate (BEZ) 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[3]. Bezafibrate was not cytotoxic against human retinal microvascular endothelial cells (HRMECs) and human retinal pigment epithelial cells (ARPE-19 cells) treated with <100 and 200μM bezafibrate, respectively. In HRMECs, the expression levels of tumor necrosis factor (TNF)-α-induced monocyte chemoattractant protein (MCP)-1, intercellular adhesion molecule (ICAM)-1, and vascular cell adhesion molecule (VCAM)-1 were significantly suppressed by bezafibrate in a dose-dependent manner. TNF-α-induced nuclear translocation of nuclear factor (NF)-κB p65 and cell migration were also significantly inhibited in bezafibrate-treated HRMECs. Furthermore, bezafibrate treatment significantly suppressed interleukin (IL)-1β-induced vascular endothelial growth factor (VEGF) production in ARPE-19 cells[4]. BEZ ameliorates diabetes probably via reduced steatosis, enhanced hepatic mitochondrial mass, improved metabolic flexibility and elevated hepatic insulin sensitivity in TallyHo mice[5]. Bezafibrate is a useful and well-tolerated lipid-modifying agent in the management of primary and secondary dyslipidaemia[6].

Bezafibrate 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02584504 Hypercholesterolemia Phase 3 Completed - Japan ... 展开 >> Investigational Site Number 392028 Ageo-Shi, Japan Investigational Site Number 392007 Chuo-Ku, Japan Investigational Site Number 392029 Chuo-Ku, Japan Investigational Site Number 392014 Fukui-Shi, Japan Investigational Site Number 392023 Hachioji-Shi, Japan Investigational Site Number 392013 Itoshima-Shi, Japan Investigational Site Number 392010 Kanazawa-Shi, Japan Investigational Site Number 392024 Kasuga-Shi, Japan Investigational Site Number 392004 Kawanishi-Shi, Japan Investigational Site Number 392015 Kitakyushu-Shi, Japan Investigational Site Number 392005 Komatsu-Shi, Japan Investigational Site Number 392032 Matsudo-Shi, Japan Investigational Site Number 392017 Matsumoto-Shi, Japan Investigational Site Number 392003 Mito-Shi, Japan Investigational Site Number 392018 Morioka-Shi, Japan Investigational Site Number 392009 Moriya-Shi, Japan Investigational Site Number 392006 Nagoya-Shi, Japan Investigational Site Number 392011 Nagoya-Shi, Japan Investigational Site Number 392019 Nagoya-Shi, Japan Investigational Site Number 392025 Nagoya-Shi, Japan Investigational Site Number 392027 Osaka-Shi, Japan Investigational Site Number 392030 Sakura-Shi, Japan Investigational Site Number 392016 Shinagawa-Ku, Japan Investigational Site Number 392001 Shinjuku-Ku, Japan Investigational Site Number 392008 Shinjuku-Ku, Japan Investigational Site Number 392012 Shizuoka-Shi, Japan Investigational Site Number 392002 Suita-Shi, Japan Investigational Site Number 392031 Suita-Shi, Japan Investigational Site Number 392020 Toyonaka-Shi, Japan Investigational Site Number 392022 Yao-Shi, Japan 收起 <<
NCT02584504 - Completed - -
NCT03031821 Prostate Cancer ... 展开 >> Metabolic Syndrome 收起 << Phase 3 Not yet recruiting June 1, 2023 Canada, British Columbia ... 展开 >> BC Cancer Agency - Vancouver Cancer Centre Not yet recruiting Vancouver, British Columbia, Canada, V5Z 4E6 Contact: Bernie Eigl, MD    604-877-6000    bernie.eigl@bccancer.bc.ca    Principal Investigator: Bernie Eigl, MD 收起 <<

Bezafibrate 参考文献

[1]Cabrero A, Alegret M, et al. Bezafibrate reduces mRNA levels of adipocyte markers and increases fatty acid oxidation in primary culture of adipocytes. Diabetes. 2001 Aug;50(8):1883-90.

[2]Krey G, Braissant O, et al. Fatty acids, eicosanoids, and hypolipidemic agents identified as ligands of peroxisome proliferator-activated receptors by coactivator-dependent receptor ligand assay. Mol Endocrinol. 1997 Jun;11(6):779-91.

[3]Willson TM, Brown PJ, Sternbach DD, Henke BR. The PPARs: from orphan receptors to drug discovery. J Med Chem. 2000 Feb 24;43(4):527-50

[4]Usui-Ouchi A, Ouchi Y, Ebihara N. 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

[5]Franko A, Neschen S, Rozman J, Rathkolb B, Aichler M, Feuchtinger A, Brachthäuser L, Neff F, Kovarova M, Wolf E, Fuchs H, Häring HU, Peter A, Hrabě de Angelis M. Bezafibrate ameliorates diabetes via reduced steatosis and improved hepatic insulin sensitivity in diabetic TallyHo mice. Mol Metab. 2017 Jan 6;6(3):256-266

[6]Goa KL, Barradell LB, Plosker GL. Bezafibrate. An update of its pharmacology and use in the management of dyslipidaemia. Drugs. 1996 Nov;52(5):725-53

Bezafibrate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.76mL

0.55mL

0.28mL

13.82mL

2.76mL

1.38mL

27.64mL

5.53mL

2.76mL

Bezafibrate 技术信息

CAS号41859-67-0
分子式C19H20ClNO4
分子量 361.819
别名 BM15075;Benzofibrate;Bezafibratum;Cedur;Difaterol;Bezatrol;Bezalip
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Store in freezer, under -20°C
溶解度

DMSO: 50 mg/mL(138.19 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: Bezafibrate | 41859-67-0 | BM15075 | BM 15075 | BM-15075 | PPAR Agonist | Cell Cycle/DNA Damage | Vitamin D Related/Nuclear Receptor | Metabolic Enzyme/Protease | PPAR | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Bezafibrate 纯度/质量文件 | Bezafibrate 亚型比较 | Bezafibrate 生物活性 | Bezafibrate 临床数据 | Bezafibrate 参考文献 | Bezafibrate 实验方案 | Bezafibrate 技术信息

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