Entacapone sodium salt is a potent, reversible, peripherally acting and orally activecatechol-O-methyltransferase (COMT)inhibitor. Entacapone sodium salt inhibitsCOMTfrom rat brain, erythrocytes and liver withIC₅₀values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone sodium salt is selective forCOMTover other catecholamine metabolizing enzymes, includingMAO-A,MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC₅₀s>50 μM). Entacapone sodium salt can be used for the research of Parkinson's disease^[1]. Entacapone sodium salt serves as as a inhibit ofFTO demethylationwith anIC₅₀of 3.5 μM, can be used for the research of metabolic disorders^[2].

IC50: 10 nM (rat brain COMT); 20 nM (rat erythrocyte COMT); 160 nM (rat liver COMT)^[1]

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^[2].

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^[2].

327.27

C₁₄H₁₄N₃NaO₅

1047659-02-8

恩他卡朋钠盐

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.