1047659-02-8
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- CAS号:
- 1047659-02-8
- 英文名:
- Entacapone (sodiuM salt)
- 英文别名:
- Entacapone Sodium;Entacapone (sodiuM salt);Sodium (E)-4-(2-cyano-3-(diethylamino)-3-oxoprop-1-en-1-yl)-2-hydroxy-6-nitrophenolate
- 中文名:
- 1047659-02-8
- 中文别名:
- 恩他卡朋钠盐;化合物 T11207;(E)-2-氰基-3-(3,4-二羟基-5-硝基苯)-N,N二乙基丙烯酰胺钠盐
- CBNumber:
- CB72681998
- 分子式:
- C14H14N3NaO5
- 分子量:
- 329.29
- MOL File:
- 1047659-02-8.mol
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1047659-02-8化学性质
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溶解度:
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Soluble in DMSO
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形态:
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Powder
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1047659-02-8性质、用途与生产工艺
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。
IC50: 10 nM (rat brain COMT); 20 nM (rat erythrocyte COMT); 160 nM (rat liver COMT)
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.
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.
1047659-02-8
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1047659-02-8, 1047659-02-8 相关搜索:
- C14H14N3NaO5
- 化合物 T11207
- (E)-2-氰基-3-(3,4-二羟基-5-硝基苯)-N,N二乙基丙烯酰胺钠盐
- 恩他卡朋钠盐
- 1047659-02-8
- Sodium (E)-4-(2-cyano-3-(diethylamino)-3-oxoprop-1-en-1-yl)-2-hydroxy-6-nitrophenolate
- Entacapone Sodium
- Entacapone (sodiuM salt)