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- 文献和实验
- 技术资料
- 保存条件:
Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
49562-28-9
- 规格:
10 mM * 1 mL/200 mg/5 g/10 g
| 规格: | 10 mM * 1 mL | 产品价格: | ¥550.0 |
|---|---|---|---|
| 规格: | 200 mg | 产品价格: | ¥390.0 |
| 规格: | 5 g | 产品价格: | ¥500.0 |
| 规格: | 10 g | 产品价格: | ¥700.0 |
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Fenofibrate
CAS No. : 49562-28-9
MCE 国际站:Fenofibrate
产品活性:Fenofibrate 是一种选择性的 PPARα 激动剂,EC50 为 30 μM。Fenofibrate 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。
研究领域:Vitamin D Related/Nuclear Receptor | Cell Cycle/DNA Damage | Metabolic Enzyme/Protease | Autophagy
作用靶点:PPAR | Cytochrome P450 | Autophagy
In Vitro: 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). 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.
In Vivo: 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.
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文献和实验特(fenofibrate) 片剂,100mg/次,3次/日,饭后服。 环丙贝特(ciprofibrate)片剂,开始100mg/次,可增至200mg/次,1次/日。 乐伐他汀(lovastatin)片剂,20~40mg/次,1次/日,晚餐时服,必要时4周内可增至80mg/次,1次/日。 普伐他汀(pravastatin) 片剂,5~10mg/次,2次/日。 塞伐他汀(simvastatin) 片剂,10mg/次,1次/日。 普罗布考(probucol) 片剂,250~500mg
非诺贝特(fenofibrate) 片剂,100mg/次,3次/日,饭后服。 环丙贝特(ciprofibrate)片剂,开始100mg/次,可增至200mg/次,1次/日。 乐伐他汀(lovastatin)片剂,20~40mg/次,1次/日,晚餐时服,必要时4周内可增至80mg/次,1次/日。 普伐他汀(pravastatin) 片剂,5~10mg/次,2次/日。 塞伐他汀(simvastatin) 片剂,10mg/次,1次/日。 普罗
酸类药效强毒性低,有吉非贝齐(gemfibrozil),苯扎贝特(bezafibrate)、非诺贝特(fenofibrate)、环丙贝特(ciprofibrate)等。 【药理作用】口服后,能明显降低病人血浆TG、VLDL、IDL含量,而使HDL升高。对LDL作用与患者血浆中TG水平有关。对单纯高甘油三酯血症患者的LDL无影响,但对单纯高胆固醇血症患者的LDL可下降15%。此外,本类药物也有抗血小板聚集、抗凝血和降低血浆粘度,增加纤溶酶活性等作用。 降低血浆TG、VLDL、IDL作用
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