
簡(jiǎn)要描述:Gemfibrozil 25812-30-0Gemfibrozil (Lopid) is an oral drug used to lower lipid levels.
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| 品牌 | absin | CAS | 25812-30-0 |
|---|---|---|---|
| 分子式 | C15H22O3 | 純度 | >98% |
| 分子量 | 250.33 | 貨號(hào) | abs47027686 |
| 規(guī)格 | 100mg | 供貨周期 | 現(xiàn)貨 |
| 主要用途 | used to lower lipid levels. | 應(yīng)用領(lǐng)域 | 化工,生物產(chǎn)業(yè),農(nóng)林牧漁,制藥/生物制藥,綜合 |
Gemfibrozil 25812-30-0
| 產(chǎn)品描述 | |
| 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. |
| 純度 | >98% |
| 儲(chǔ)存/保存方法 | Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 別名 | 吉非luo齊;CI-719 |
| 外觀 | 白色粉末 |
| 可溶性/溶解性 | DMSO : 47 mg/mL (187.8 mM) Ethanol : 47 mg/mL (187.8 mM) |
| 生物活性 | |
| 靶點(diǎn) | PPARα |
| In vitro(體外研究) | 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. |
| In vivo(體內(nèi)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. |
| 參考文獻(xiàn) | |
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| 研究領(lǐng)域 | |
| 研究領(lǐng)域 | CardiovascularLipids / LipoproteinsLipid MetabolismCytochromes MetabolismPathways and ProcessesMetabolic signaling pathwaysDrug metabolism MetabolismPathways and ProcessesMetabolic signaling pathwaysLipid and lipoprotein metabolismLipases MetabolismPathways and ProcessesMitochondrial MetabolismCytochromes NeuroscienceDevelopment NeuroscienceProcesses Signal TransductionMetabolismDrug metabolism Signal TransductionMetabolismLipid metabolism Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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