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1047659-02-8

中文名称 1047659-02-8
英文名称 Entacapone (sodiuM salt)
CAS 1047659-02-8
分子式 C14H14N3NaO5
分子量 329.29
MOL 文件 1047659-02-8.mol
1047659-02-8 结构式 1047659-02-8 结构式

基本信息

中文别名
恩他卡朋钠盐
英文别名
Entacapone Sodium
Entacapone (sodiuM salt)

物理化学性质

溶解度Soluble in DMSO
形态Powder

安全数据

危险性符号(GHS)GHS hazard pictograms
GHS06
警示词危险
危险性描述H301

常见问题列表

生物活性
Entacapone sodium salt 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 sodium salt 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 sodium salt 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 sodium salt 可用于帕金森病的研究。Entacapone sodium salt 抑制 FTO 去甲基化活性,IC50 是 3.5 μM,可用于研究代谢紊乱。
靶点

IC50: 10 nM (rat brain COMT); 20 nM (rat erythrocyte COMT); 160 nM (rat liver COMT)

体外研究

Entacapone sodium salt (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 sodium salt -treated Hep-G2 cells.

体内研究

Entacapone sodium salt (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 sodium salt treatment. Entacapone sodium salt 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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