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Fenofibrate

Fenofibrate

产品编号 T1149   CAS 49562-28-9
别名: Procetofen, 非诺贝特, Lipanthyl, Lipantil

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。

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Fenofibrate Chemical Structure
Fenofibrate, CAS 49562-28-9
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
产品目录号及名称: Fenofibrate (T1149)
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纯度: 99.97%
纯度: 99.95%
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生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

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

溶解度

Ethanol: 36.1 mg/mL (100 mM)

DMSO: 36.1 mg/mL (100 mM)

溶液配制表

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

计算器

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稀释计算器
配液计算器
分子量计算器
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参考文献

1. Schelleman H, et al. Pharmacoepidemiologic and in vitro evaluation of potential drug-drug interactions of sulfonylureas with fibrates and statins. Br J Clin Pharmacol. 2014 Sep;78(3):639-48. 2. Gong Y, et al. Fenofibrate Inhibits Cytochrome P450 Epoxygenase 2C Activity to Suppress Pathological Ocular Angiogenesis. EBioMedicine. 2016 Sep 30. pii: S2352-3964(16)30448-0. 3. Kong R, Wang N, Han W, et al. Fenofibrate Exerts Antitumor Effects in Colon Cancer via Regulation of DNMT1 and CDKN2A[J]. PPAR research. 2021, 2021. 4. Zeng X, Zhu S, Lu W, et al. Target identification among known drugs by deep learning from heterogeneous networks[J]. Chemical Science. 2020, 11(7): 1775-1797.

文献引用

1. Zeng X, Zhu S, Lu W, et al. Target identification among known drugs by deep learning from heterogeneous networks. Chemical Science. 2020, 11(7): 1775-1797. 2. Zhang Y, Li T, Pan M, et al. SIRT1 prevents cigarette smoking-induced lung fibroblasts activation by regulating mitochondrial oxidative stress and lipid metabolism. Journal of Translational Medicine. 2022, 20(1): 1-13 3. Kong R, Wang N, Han W, et al. Fenofibrate Exerts Antitumor Effects in Colon Cancer via Regulation of DNMT1 and CDKN2A. PPAR research. 2021, 2021.
RG-12525 LJ570 MA-0204 Indeglitazar Rosiglitazone hydrochloride Eupatilin U-46619 Astaxanthin

相关化合物库

该产品包含在如下化合物库中:
抗癌临床化合物库 神经退行性疾病化合物库 抗癌药物库 抗癌上市药物库 抗衰老化合物库 人代谢物化合物库 经典已知活性库 抗心血管疾病化合物库 抗糖尿病库 临床期小分子药物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
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每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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% ddH2O
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技术支持

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。

Keywords

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

 

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