您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > Cycloguanil(hydrochloride)
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:
 
Cycloguanil(hydrochloride)
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。
Cycloguanil(hydrochloride)图片
CAS NO:152-53-4
包装与价格:
包装价格(元)
10mg电议
25mg电议
50mg电议

产品介绍

化学性质

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt288.2
Cas No.152-53-4
FormulaC11H14ClN5·HCl
SynonymsChloroguanide Triazine,NSC 3074
Solubility≤5mg/ml in ethanol;20mg/ml in DMSO;5mg/ml in dimethyl formamide
Chemical Name1-(4-chlorophenyl)-1,6-dihydro-6,6-dimethyl-1,3,5-triazine-2,4-diamine, monohydrochloride
Canonical SMILESClC1=CC=C(N2C(N)=NC(N)=NC2(C)C)C=C1.Cl
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

Cycloguanil is an inhibitor of dihydrofolate reductase (DHFR)[1].

Dihydrofolate reductase (DHFR) is an enzyme that involved in reducing dihydrofolic acid to tetrahydrofolic acid. DHFR plays a critical role in regulating the amount of tetrahydrofolate in the cell, which are essential for purine and thymidylate synthesis important for cell proliferation and cell growth. DHFR also plays a central role in the synthesis of nucleic acid precursors and salvage of tetrahydrobiopterin from dihydrobiopterin [2].

Cycloguanil is the active metabolite of proguanil produced by the cytochrome P450 (CYP) [3]. Cycloguanil showed activity against P. falciparu. Cycloguanil inhibited the activity of dihydrofolate reductase (DHFR) with the Ki values of 0.3 and 1.5 nM for Plasmodium and human forms, respectively., Cycloguanil prevented the production of tetrahydrofolic acid, an essential coenzyme involved in DNA and RNA synthesis, by blocking DHFR activity.

References:
[1] Foote S J, Galatis D, Cowman A F.  Amino acids in the dihydrofolate reductase-thymidylate synthase gene of Plasmodium falciparum involved in cycloguanil resistance differ from those involved in pyrimethamine resistance[J]. Proceedings of the National Academy of Sciences, 1990, 87(8): 3014-3017.
[2] Blakley R L.  Dihydrofolate reductase[J]. Encyclopedia Of Molecular Medicine, 1984.
[3] Birkett D J, Rees D, Andersson T, et al.  In vitro proguanil activation to cycloguanil by human liver microsomes is mediated by CYP3A isoforms as well as by S‐mephenytoin hydroxylase[J]. British journal of clinical pharmacology, 1994, 37(5): 413-420.