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Fenofibrate

CAS No. : 49562-28-9

MCE 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：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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