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Entacapone
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Entacapone图片
CAS NO:130929-57-6
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议
100mg电议

产品介绍
Entacapone 是一种有效的、可逆的、外周作用和口服活性的儿茶酚-O-甲基转移酶 (COMT) 抑制剂。
Cas No.130929-57-6
别名恩他卡朋
化学名(E)-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N,N-diethylprop-2-enamide
Canonical SMILESCCN(CC)C(=O)C(=CC1=CC(=C(C(=C1)O)O)[N+](=O)[O-])C#N
分子式C14H15N3O5
分子量305.29
溶解度≥ 13.1 mg/mL in DMSO, ≥ 12.65 mg/mL in EtOH with ultrasonic
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
文献引用
产品描述

Entacapone is a second-generation catechol-O-methyltransferase (COMT) inhibitor that potently inhibits rat liver total COMT with the half maximal inhibition concentration IC50 and inhibition constant Ki values of 20.1 nM and 10.7 nM respectively. The IC50 values of entacapone against rate liver soluble COMT (S-COMT) and rat liver membrane-bound COMT (MB-COMT) are 14.3 nM and 73.3 nM respectively [1].

Entacapone has succbe used as an adjunct to standard levodopa-dopa decarboxylase inhibitor therapy in patients with Parkinson’s disease (PD), for its abilities to increase the bioavailability of levodopa by inhibiting the generation of 3-O-methyldopa and to prolong the duration and clinical benefit of levodopa [1].

Reference

References:
[1] Forsberg M, Lehtonen M, Heikkinen M, Savolainen J, Jarvinen T, Mannisto PT. Pharmacokinetics and pharmacodynamics of entacapone and tolcapone after acute and repeated administration: a comparative study in the rat. J Pharmacol Exp Ther. 2003 Feb;304(2):498-506.