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1047659-02-8

中文名稱 1047659-02-8
CAS 1047659-02-8
分子式 C14H14N3NaO5
1047659-02-8 結(jié)構(gòu)式 1047659-02-8 結(jié)構(gòu)式

基本信息

中文別名
恩他卡朋鈉鹽
英文別名
Entacapone Sodium
Entacapone (sodiuM salt)

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS06
警示詞危險(xiǎn)
危險(xiǎn)性描述H301

常見(jiàn)問(wèn)題列表

生物活性
Entacapone sodium salt 是一種有效的、可逆的、外周作用和具有口服活性兒茶酚-O-甲基轉(zhuǎn)移酶 (COMT) 抑制劑。Entacapone sodium salt 對(duì)大鼠腦、紅細(xì)胞和肝臟 COMT 有抑制作用,IC50 值分別為 10 nM、20 nM 和 160 nM。Entacapone sodium salt 對(duì) COMT 的選擇性優(yōu)于其他兒茶酚胺代謝酶,包括MAO-A、MAO-B、酚磺基轉(zhuǎn)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,可用于研究代謝紊亂。
靶點(diǎn)

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

體外研究

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.

體內(nèi)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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