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Fenofibrate Sale

(Synonyms: 非诺贝特) 目录号 : GC12250

A PPARα agonist

Fenofibrate Chemical Structure

Cas No.:49562-28-9

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥385.00
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200mg
¥273.00
现货
5g
¥350.00
现货
10g
¥490.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Cell experiment [1]:

Cell lines

MCF-7 and Panc-1 cells

Preparation method

The solubility of this compound in DMSO is > 12.8 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

24, 48 and 72 hrs

Applications

At 24th, 48th and 72th hrs, the IC50 values of Fenofibrate were 96.6, 46.5 and 9.2 μg/mL on Panc-1 cells, and 93.5, 55.9 and 8 μg/mL on MCF-7 cells, respectively. Compared with the untreated solvent control, MCF-7 and Panc-1 cells treated with 1/2 IC50, IC50 and 2 IC50 of Fenofibrate for 24 hrs exhibited a significant increase in the relative activity of caspase 3/7.

Animal experiment [1]:

Animal models

Mice bearing Ehrlich ascites carcinoma (EAC)

Dosage form

200 mg/kg/day; p.o.; for 18 days

Applications

In an EAC mouse model, Fenofibrate significantly reduced tumor weight and volume, without affecting the relative heart weight. However, Fenofibrate treatment significantly decreased the body weight and increased the relative liver weight. In addition, a marked decrease in the carcinoembryonic antigen (CEA) level was also observed in the Fenofibrate treatment group.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Sabaa M, ELFayoumi HM, Elshazly S, Youns M, Barakat W. Anticancer activity of salicin and fenofibrate. Naunyn Schmiedebergs Arch Pharmacol. 2017 Jul 21.

产品描述

Fenofibrate is a PPARα agonist with an EC50 of 30 μM.

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].

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].

References:
[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.

Chemical Properties

Cas No. 49562-28-9 SDF
别名 非诺贝特
化学名 propan-2-yl 2-[4-(4-chlorobenzoyl)phenoxy]-2-methylpropanoate
Canonical SMILES CC(C)OC(=O)C(C)(C)OC1=CC=C(C=C1)C(=O)C2=CC=C(C=C2)Cl
分子式 C20H21ClO4 分子量 360.83
溶解度 ≥ 12.75mg/mL in DMSO 储存条件 Store at RT
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.7714 mL 13.8569 mL 27.7139 mL
5 mM 0.5543 mL 2.7714 mL 5.5428 mL
10 mM 0.2771 mL 1.3857 mL 2.7714 mL
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