Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Fenofibrate (Lipanthyl) 是一种选择性PPARα激动剂,EC50为 30 μM。它是一种合成的苯氧基异丁酸衍生物和前药,具有抗高血脂活性。它抑制细胞色素 P450 亚型, 对CYP2C19、CYP2B6、CYP2C9、CYP2C8和CYP3A4的IC50分别为 0.2、0.7、9.7、4.8 和 142.1 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
100 mg | ¥ 168 | 现货 | ||
200 mg | ¥ 318 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 384 | 现货 |
产品描述 | Fenofibrate (Lipanthyl) is a peroxisome proliferator receptor alpha agonist. Fenofibrate is a synthetic phenoxy-isobutyric acid derivate and prodrug with antihyperlipidemic activity. |
靶点活性 | PPARα:30 μM(EC50) |
体外活性 | Fenofibrate is a relatively potent inhibitor of CYP2B6 (IC50=0.7±0.2 μM) and CYP2C19 (IC50=0.2±0.1 μM). Fenofibrate is also a moderate inhibitor of CYP2C8 (IC50=4.8±1.7 μM) and CYP2C9 (IC50=9.7 μM)[1]. Fenofibrate binds to and inhibits cytochrome P450 epoxygenase (CYP)2C with higher affinity than to PPARα. Fenofibrate is a well-known PPARα agonist, but an in vitro assessment of 209 frequently prescribed drugs and related xenobiotics suggests that Fenofibrate is also a potent inhibitor of cytochrome P450 epoxygenase (CYP)2C. The affinity of Fenofibrate to CYP2C is >10 times higher (EC50=2.39±0.4 μM) than to PPARα (EC50=30 μM). Fenofibrate at a low dose inhibits CYP2C8 activity without PPARα activation[2]. |
体内活性 | Daily intake of Fenofibrate at this low dose (10 μg/g/day) inhibits retinal and choroidal neovascularization induced by CYP2C8 overexpression by 29% (P=0.021) and 36% (P=1.2×10?9) respectively[2]. |
激酶实验 | The half-maximal inhibitory concentrations (IC50s) of Fenofibrate, statins (atorvastatin, lovastatin, pravastatin, simvastatin and simvastatin acid, the active form of simvastatin) and glipizide for recombinant human CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and CYP3A4 are determined using fluorometric CYP450 inhibition assays. Briefly, the drugs are dissolved in methanol or acetonitrile. In 96 well assay plates, the drugs are diluted to a series of concentrations in a solution containing cofactors including NADP+ (final concentration 1.3 mM), MgCl2 (final concentration 3.3 m M), glucose-6-phosphate (G6P, final concentration 3.3 mM) and glucose 6-phosphate dehydrogenase (final concentration 0.4 U/mL). The mixture is pre-incubated at 37°C for 10 min. The enzymes and fluorogenic substrates are diluted to desired concentrations in sodium phosphate reaction buffer (pH 7.4, final concentration 200 mM) and mixed. Reactions are initiated with addition of the enzyme and substrate mixture to the cofactor and drug mixture. The final reaction volume of all assays is 200 μL. After incubating at 37°C for a pre-specified period of time (15 to 45 min), the reactions are stopped with addition of 75 μL quenching solution (0.5 M Tris base or 2N NaOH). Fluorescence is determined using a BioTek Synergy 2 fluorescence reader. Each of the drugs is tested at eight concentrations in duplicate. To estimate IC50s, percent of inhibition is calculated using net fluorescence that is corrected for the background. The values of percent of inhibition are then fitted to a three or four parameter log-logistic model[1]. |
别名 | Procetofen, 非诺贝特, Lipanthyl, Lipantil |
分子量 | 360.83 |
分子式 | C20H21ClO4 |
CAS No. | 49562-28-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 36.1 mg/mL (100 mM)
DMSO: 36.1 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.7714 mL | 13.8569 mL | 27.7139 mL | 69.2847 mL |
5 mM | 0.5543 mL | 2.7714 mL | 5.5428 mL | 13.8569 mL | |
10 mM | 0.2771 mL | 1.3857 mL | 2.7714 mL | 6.9285 mL | |
20 mM | 0.1386 mL | 0.6928 mL | 1.3857 mL | 3.4642 mL | |
50 mM | 0.0554 mL | 0.2771 mL | 0.5543 mL | 1.3857 mL | |
100 mM | 0.0277 mL | 0.1386 mL | 0.2771 mL | 0.6928 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Fenofibrate 49562-28-9 Autophagy DNA Damage/DNA Repair Metabolism P450 PPAR Procetofen inhibit 非诺贝特 Peroxisome proliferator-activated receptors Lipanthyl Lipantil CYPs Cytochrome P450 Inhibitor inhibitor