货号 | 4720/10 |
别名 | (2E)-2-Cyano-3-(3,4-dihydroxy-5-nit |
供应商 | Tocris |
生物活性 | Potent catechol O-methyltransferase (COMT) inhibitor (IC50 values are 14.3, 20.1 and 73.3 nM for rat liver soluble COMT, total COMT and membrane-bound COMT respectively). Increases bioavailability of levodopa when given as an adjunct therapy for Parkinson's disease. Inhibits α-synuclein aggregation in an in vitro assay; blocks α-synuclein-induced cell death in PC-12 cells. |
运输条件 | Blue Ice |
存放说明 | Ambient |
纯度 | >99 % |
计算分子量 | 305.29 |
分子式 | C14H15N3O5 |
可溶性/溶解性 | Soluble to 100 mM in DMSO and to 10 mM in ethanol |
参考文献 | Di Giovanniet al (2010) Entacapone and tolcapone, two catechol O-methyltransferase inhibitors, block fibril formation of alpha-synuclein and beta-amyloid and protect against amyloid-induced toxicity. J.Biol.Chem. 285 14941. PMID: 20150427. Forsberget al (2003) Pharmacokinetics and pharmacodynamics of entacapone and tolcapone after acute and repeated administration: a comparative study in the rat. J.Pharmacol.Exp.Ther. 304 498. PMID: 12538800. Merelloet al (1994) Effect of entacapone, a peripherally acting catechol-O-methyltransferase inhibitor, on the motor response to acute treatment with levodopa in patients with Parkinsons disease. J.Neurol.Neurosurg.Psychiatry 57 186. PMID: 8126502. |