| Bioactivity | Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone 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 can be used for the research of Parkinson's disease[1]. Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders[2]. | ||||||||||||
| Target | IC50: 10 nM (rat brain COMT); 20 nM (rat erythrocyte COMT); 160 nM (rat liver COMT) | ||||||||||||
| Invitro | 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[2]. | ||||||||||||
| 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[2]. Animal Model: | ||||||||||||
| Name | Entacapone | ||||||||||||
| CAS | 130929-57-6 | ||||||||||||
| Formula | C14H15N3O5 | ||||||||||||
| Molar Mass | 305.29 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. E Nissinen, et al. Biochemical and pharmacological properties of a peripherally acting catechol-O-methyltransferase inhibitor entacapone. Naunyn Schmiedebergs Arch Pharmacol. 1992 Sep;346(3):262-6. [2]. Shiming Peng, et al. Identification of entacapone as a chemical inhibitor of FTO mediating metabolic regulation through FOXO1. Sci Transl Med |
Entacapone
CAS: 130929-57-6 F: C14H15N3O5 W: 305.29
Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor.
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