Gemfibrozil,25812-30-0

公告提醒：爱必信所有产品和服务仅用于科学研究，不用于临床应用及其他用途提供产品和服务（也不为任何个人提供产品和服务）!

YZ剂描述：

产品名称：Gemfibrozil

产品别名：吉非罗齐

英文别名：CI-719

靶点：PPARα

CAS：25812-30-0

纯度：＞98%

外观：白色粉末

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

Gemfibrozil (Lopid) is an oral drug used to lower lipid levels. It belongs to a group of drugs known as fibrates. Increases activity of Peroxisome proliferator-activated receptor-alpha (PPARα) 'transcription factor ligand' , a receptor that is involved in metabolism of carbohydrates and fats, as well as adipose tissue differentiation. This increase in the synthesis of lipoprotein lipase thereby increases the clearance of triglycerides.

溶解性：DMSO : 47 mg/mL (187.8 mM)
Ethanol : 47 mg/mL (187.8 mM)

体外研究：

Gemfibrozil exerts a minimal inhibitory effect on CYP3A-mediated simvastatin hydroxy acid (SVA) oxidation, but does inhibit SVA glucuronidation in dog and human liver microsomes. Gemfibrozil markedly inhibits M-23 formation, with a K(i) (IC(50)) value of 69 (95) mM, whereas inhibition of M-1 formation is weaker with a K(i) (IC(50)) value of 273 mM in human liver microsomes. Gemfibrozil strongly and competitively inhibits CYP2C9 activity, with a K(i) (IC(50)) value of 5.8 (9.6) mM. Gemfibrozil exhibits somewhat smaller inhibitory effects on CYP2C19 and CYP1A2 activities, with K(i) (IC(50)) values of 24 (47) mM and 82 (136) mM, respectively. Gemfibrozil, a lipid-lowering drug, inhibits cytokine-induced production of NO and the expression of inducible nitric-oxide synthase (iNOS) in human U373MG astroglial cells and primary astrocytes. Gemfibrozil induces peroxisome proliferator-responsive element (PPRE)-dependent luciferase activity, which is inhibited by the expression of DeltahPPAR-alpha, the dominant-negative mutant of human PPAR-alpha. Gemfibrozil strongly inhibits the activation of NF-kappaB, AP-1, and C/EBPbeta but not that of gamma-activation site (GAS) in cytokine-stimulated astroglial cells.

体内研究：Gemfibrozil treatment significantly reduces (2-3-fold) the plasma clearance of SVA and the biliary excretion of SVA glucuronide (together with its cyclization product SV), but not the excretion of a major oxidative metabolite of SVA in dogs.

产品信息订购：

产品更多信息请进入爱必信网站咨询