| 货号 | 14835-1g |
| 描述 | Gemfibrozil is a fibrate that activates peroxisome proliferator-activator α (PPARα, EC50 = 193 μM) with 100% efficacy.1 It also activates PPARγ (EC50 = 148 μM), but with only 79% efficacy.1 Presumably through its effects on PPARα, gemfibrozil lowers triglycerides and increases high density lipoprotein cholesterol levels and is used in the context of atherogenic dyslipidemia.2 Gemfibrozil strongly binds liver fatty acid-binding protein (Ki = 1.8 μM).3 Phase II metabolites of gemfibrozil inhibit certain cytochrome P450 isoforms, increasing drug-drug interaction risks.4 |
| 别名 | CI-719;Lopid; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Kim, N.J.,Lee, K.O.,Koo, B.W., et al. Design, synthesis, and structure-activity relationship of carbamate-tethered aryl propanoic acids as novel PPARα/γ dual agonists. Bioorganic & Medicinal Chemistry Letters 17(13), 3595-3598 (2007). 2.Tenenbaum, A. and Fisman, E.Z. Fibrates are an essential part of modern anti-dyslipidemic arsenal: Spotlight on atherogenic dyslipidemia and residual risk reduction. Cardiovascular Diabetology 11, 125 (2012). 3.Chuang, S.,Velkov, T.,Horne, J., et al. Characterization of the drug binding specificity of rat liver fatty acid binding protein. Journal of Medicinal Chemistry 51(13), 3755-3764 (2008). 4.Orr, S.T.M.,Ripp, S.L.,Ballard, T.E., et al. Mechanism-based inactivation (MBI) of cytochrome P450 enzymes: Structure-activity relationships and discovery strategies to mitigate drug-drug interaction risks. Journal of Medicinal Chemistry 55(11), 4896-4933 (2012). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 250.3 |
| 分子式 | C15H22O3 |
| CAS号 | 25812-30-0 |
| 稳定性 | ≥ 2 years |
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