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Entacapone

CAS No. : 130929-57-6

MCE 国际站：Entacapone

产品活性：Entacapone 是一种有效的、可逆的、外周作用和具有口服活性儿茶酚-O-甲基转移酶 (COMT) 抑制剂。Entacapone 对大鼠脑、红细胞和肝脏 COMT 有抑制作用，IC₅₀ 值分别为 10 nM、20 nM和160 nM。Entacapone 对 COMT 的选择性优于其他儿茶酚胺代谢酶，包括MAO-A、MAO-B、酚磺基转移酶 M (PST-M) 和 PST-P (IC₅₀s >50 µM)。Entacapone 可用于帕金森病的研究。Entacapone 抑制 FTO 去甲基化活性，IC₅₀ 是 3.5 μM，可用于研究代谢紊乱。

研究领域：Metabolic Enzyme/Protease  |  Neuronal Signaling

作用靶点：COMT

In Vitro: Entacapone (50 μM, 48 hours) enhances the amount of m6A on mRNA in Hep-G2 cells. It does not show any inhibitory effect on the enzymatic activity of the RNA m6A demethylase AlkB homolog 5 (ALKBH5) or the ten-eleven translocation methylcytosine dioxygenase 1 (TET1), nor does it alter the DNA methylation or histone methylation patterns in entacapone-treated Hep-G2 cells.

In Vivo: Entacapone (oral administration; 600 mg/kg per day; 3-9 weeks) results in a dose-response effect dose-response effect. After 3 weeks, mouse body weight are decreased by 10.1% compared to controls, and shows similar food intake  fat mass and fat mass ratio reduced after entacapone treatment. Entacapone also increases the energy expenditure of mice: reductions in total cholesterol (17.6%), low-density lipoprotein cholesterol (31.0%), and triglycerides (10.2%) in mice.

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