Entacapone

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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 is a selective, reversible catechol-O-methyl transferase (COMT) inhibitor for the treatment of Parkinson's disease. It is a member of the class of nitrocatechols. When administered concomittantly with levodopa and a decarboxylase inhibitor (e.g., carbidopa), increased and more sustained plasma levodopa concentrations are reached as compared to the administration of levodopa and a decarboxylase inhibitor. (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.

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.

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. Animal Model:High-fat diet-induced obese (DIO) mouse model Dosage:600 mg/kg Administration:Oral administration; 600 mg/kg per day; 3-9 weeks Result:Regulated the metabolic disorders in DIO mouse.

OR-611

Metabolic Enzyme/Protease

Transferase

COMT

Neurological Disease

——

130929-57-6

305.29

C14H15N3O5

>98% (HPLC)

Ethanol: 2 mg/mL (6.55 mM); DMSO: 61 mg/mL (199.81 mM)

O=C(N(CC)CC)/C(C#N)=C/C1=CC([N+]([O-])=O)=C(O)C(O)=C1

(E)-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N,N-diethylacrylamide

(-20℃)

With Ice Pack

≥ 2 years