您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > Hydroxytacrine(maleate)
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Hydroxytacrine(maleate)
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。
Hydroxytacrine(maleate)图片
CAS NO:118909-22-1
包装与价格:
包装价格(元)
250mg电议
1g电议

产品介绍

化学性质

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt330.3
Cas No.118909-22-1
FormulaC13H14N2O·C4H4O4
SynonymsHP 029,1-Hydroxytacrine,P 83-6029A,Velnacrine
Solubility≤30mg/ml in DMSO;2mg/ml in dimethyl formamide
Chemical Name9-amino-1,2,3,4-tetrahydro-1-acridinol, 2Z-butenedioate
Canonical SMILESNC1=C2C(CCCC2O)=NC3=CC=CC=C31.OC(/C=C\C(O)=O)=O
运输条件蓝冰运输或根据您的需求运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。

资料参考

Hydroxytacrine maleate, a bioactive monohydroxylated metabolite of cholinesterase inhibitor, is a potential Alzheimer's therapeutic of low toxicity [1]. Hydroxytacrine maleate exhibited biochemical and pharmacological profile similar to tacrine (THA) except that the far less liver toxicity in humans. The prolonged use of tacrine has been associated with liver toxicity[1, 2].

Hydroxytacrine maleate is a parasympathomimetic and a centrally acting cholinesterase inhibitor (anticholinesterase). As the first cholinesterase inhibitor approved for the treatment of AD, tacrine was marketed under the trade name Cognex [3]. Through hydroxylation of benzylic carbon by CYP450 in the liver, tacrine has been metabolized into metabolite 1-hydroxy-tacrine (velnacrine) [4]. It has also been shown that maleate is an inhibitor of AChE [5].

References:
[1].  D. Muoz-Torrero. Acetylcholinesterase inhibitors as disease-modifying therapies for Alzheimer’s disease. Curr. Med. Chem. 15, 2433-2455 (2008).
[2].  E. Giacobini. Cholinesterase inhibitors for Alzheimer’s disease therapy: From tacrine to future applications. Neurochemistry International 32, 413-419(1998).
[3].  Birks J S. Cholinesterase inhibitors for Alzheimer's disease[J]. The Cochrane Library, 2006.
[4].  Peng J Z, Remmel R P, Sawchuk R J. Inhibition of murine cytochrome P4501A by tacrine: in vitro studies[J]. Drug metabolism and disposition, 2004, 32(8): 805-812.
[5].  Acetylcholine and choline effects on erythrocyte nitrite and nitrate levels.