Entacapone sodium salt 

Entacapone sodium salt is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone sodium salt inhibits COMT from rat brain, erythrocytes and liver with IC₅₀ values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone sodium salt is selective for COMT over other catecholamine metabolizing enzymes, including MAO-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 of FTO demethylation with an IC₅₀ of 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

327.27

C₁₄H₁₄N₃NaO₅

1047659-02-8

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

Room temperature in continental US; may vary elsewhere.

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

• [1]. E Nissinen, et al. Biochemical and pharmacological properties of a peripherally acting catechol-O-methyltransferase inhibitor Entacapone sodium salt . Naunyn Schmiedebergs Arch Pharmacol. 1992 Sep;346(3):262-6.  [Content Brief]

  [2]. Shiming Peng, et al. Identification of Entacapone sodium salt as a chemical inhibitor of FTO mediating metabolic regulation through FOXO1. Sci Transl Med  [Content Brief]