非诺贝特 T1149

Product Introduction
Bioactivity


英文名: Fenofibrate

描述: 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。

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].

体外活性: Fenofibrate 是一种相对强效的CYP2B6（IC50=0.7±0.2 μM）和CYP2C19（IC50=0.2±0.1 μM）抑制剂，并且对CYP2C8（IC50=4.8±1.7 μM）和CYP2C9（IC50=9.7 μM）也有中等抑制作用[1]。Fenofibrate 比对PPARα的结合亲和力更高地结合并抑制细胞色素P450环氧化酶（CYP）2C。作为众所周知的PPARα激动剂，Fenofibrate 在对209种常用化合物及相关外源性化合物的体外评估中显示出对细胞色素P450环氧化酶（CYP）2C的显著抑制作用。Fenofibrate 对CYP2C的亲和力是对PPARα的>10倍（EC50=2.39±0.4 μM与EC50=30 μM）。低剂量的Fenofibrate 可抑制CYP2C8活性，而不激活PPARα[2]。

体内活性: 日常摄入低剂量Fenofibrate（10 μg/g/天）可抑制由CYP2C8过表达引起的视网膜和脉络膜新生血管化的概率分别为 29%（P=0.021）和36%（P=1.2×10^-9）[2]。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 36.1 mg/mL (100 mM)
DMSO : 55 mg/mL (152.43 mM)


关键字: PPAR | inhibit | Peroxisome proliferator-activated receptors | CYPs | Cytochrome P450 | Autophagy | Fenofibrate | Inhibitor

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相关库: FDA-Approved Drug Library | Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | Drug-induced Liver Injury (DILI) Compound Library | Anti-Cancer Drug Library | Anti-Cancer Clinical Compound Library | Anti-Obesity Compound Library | Pediatric Drug Library | Anti-Cancer Approved Drug Library | EMA Approved Drug Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途