| Identification | Back Directory | [Name]
Entacapone (sodiuM salt) | [CAS]
1047659-02-8 | [Synonyms]
Entacapone Sodium
Entacapone (sodiuM salt) | [Molecular Formula]
C14H14N3NaO5 | [MDL Number]
MFCD28346924 | [MOL File]
1047659-02-8.mol | [Molecular Weight]
329.29 |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
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]. | [References]
[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. DOI:10.1007/BF00173538
[2] Shiming Peng, et al. Identification of Entacapone sodium salt as a chemical inhibitor of FTO mediating metabolic regulation through FOXO1. Sci Transl Med DOI:10.1126/scitranslmed.aau7116 |
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