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吉非罗齐 /Gemfibrozil {[allProObj[0].p_purity_real_show]}

货号:A640007 同义名: CI-719

Gemfibrozil is an agonist of PPARα. It can act as a hyperlipidemic agent that elevates plasma HDL and lowers triglycerides.

Gemfibrozil 化学结构 CAS号:25812-30-0
Gemfibrozil 化学结构
CAS号:25812-30-0
Gemfibrozil 3D分子结构
CAS号:25812-30-0
Gemfibrozil 化学结构 CAS号:25812-30-0
Gemfibrozil 3D分子结构 CAS号:25812-30-0
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Gemfibrozil 纯度/质量文件 产品仅供科研

货号:A640007 标准纯度: {[allProObj[0].p_purity_real_show]}
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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。

Gemfibrozil 生物活性

描述 PPAR (peroxisome proliferator-activated receptors) are ligand-activated transcription factors of nuclear hormone receptor superfamily comprising of PPARα, PPARγ, and PPARβ/δ[3]. Gemfibrozil is a PPARα and PPARγ agonist (EC50s = 193.3 and 147.8 µM, respectively)[4]. In vivo, gemfibrozil (50 mg/kg, p.o.) reduces serum total cholesterol, triglyceride, and LDL levels in a rat model of high-cholesterol diet-induced hyperlipidemia[5]. Gemfibrozil (100 mg/kg per day) reduces atherosclerotic plaque area, superoxide production, and expression of the genes encoding the NF-κB subunit p65 and chemokine (C-C) motif ligand 2 (CCL2) in ApoE-/- mice. Formulations containing gemfibrozil have been used in the treatment of high cholesterol[6].

Gemfibrozil 参考文献

[1]Pahan K, Jana M, et al. Gemfibrozil, a lipid-lowering drug, inhibits the induction of nitric-oxide synthase in human astrocytes. J Biol Chem. 2002;277(48):45984-91

[2]Prueksaritanont T, Zhao JJ, et al. Mechanistic studies on metabolic interactions between gemfibrozil and statins. J Pharmacol Exp Ther. 2002 Jun;301(3):1042-51.

[3]Tyagi S, Gupta P, Saini AS, Kaushal C, Sharma S. The peroxisome proliferator-activated receptor: A family of nuclear receptors role in various diseases. J Adv Pharm Technol Res. 2011 Oct;2(4):236-40.

[4]Kim NJ, Lee KO, Koo BW, et al. Design, synthesis, and structure-activity relationship of carbamate-tethered aryl propanoic acids as novel PPARalpha/gamma dual agonists. Bioorg Med Chem Lett. 2007;17(13):3595-3598.

[5]Solanki YB, Jain SM. Antihyperlipidemic activity of Clitoria ternatea and Vigna mungo in rats. Pharm Biol. 2010;48(8):915-923.

[6]Calkin AC, Cooper ME, Jandeleit-Dahm KA, Allen TJ. Gemfibrozil decreases atherosclerosis in experimental diabetes in association with a reduction in oxidative stress and inflammation. Diabetologia. 2006;49(4):766-774.

Gemfibrozil 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.99mL

0.80mL

0.40mL

19.97mL

3.99mL

2.00mL

39.95mL

7.99mL

3.99mL

Gemfibrozil 技术信息

CAS号25812-30-0
分子式C15H22O3
分子量 250.33
别名 CI-719
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,Room Temperature

溶解度

DMSO: 105 mg/mL(419.45 mM),配合低频超声助溶,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
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