Entacapone sodium is a specific, potent, peripherally acting catechol-O-methyltransferase (COMT) inhibitor with IC50 of 151 nM for PD treatment.
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Entacapone sodium salt is an effective, reversible, peripherally active, and orally administered catechol-O-methyltransferase (COMT) inhibitor. It inhibits COMT in rat brain, erythrocytes, and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone sodium salt selectively inhibits COMT over other catecholamine metabolizing enzymes such as MAO-A, MAO-B, phenolsulphotransferase M (PST-M), and PST-P, all with IC50 values greater than 50 µM, and is used in Parkinson's disease research[1]. Entacapone sodium salt acts as an inhibitor of FTO demethylation with an IC50 of 3.5 μM and is utilized in metabolic disorder studies[2].
体内研究
Entacapone sodium salt, administered orally at 600 mg/kg per day for 3-9 weeks, shows a dose-response effect. After three weeks, it reduces mouse body weight by 10.1% compared to controls without affecting food intake, reduces fat mass and fat mass ratio, and enhances energy expenditure. It also decreases total cholesterol by 17.6%, low-density lipoprotein cholesterol by 31.0%, and triglycerides by 10.2% in mice[2].
体外研究
Entacapone sodium salt, at 50 μM for 48 hours, increases m6A levels on mRNA in Hep-G2 cells. It does not inhibit the activities of RNA m6A demethylase ALKBH5 or ten-eleven translocation methylcytosine dioxygenase 1 (TET1), nor does it change DNA or histone methylation patterns in treated Hep-G2 cells[2].
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