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WR-99210
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。
WR-99210图片
CAS NO:30711-93-4
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6,6-Dimethyl-1-[3-(2,4,5-trichlorophenoxy)propoxy]-1,6-dihydro-1,3,5-triazine-2,4-diamine
WR99210 hydrochloride(47326-86-3 free base)
WR-99210 是恶性疟原虫二氢叶酸还原酶 (pfDHFR) 的有效抑制剂,pfDHFR 是主要的疟疾药物靶点。它对野生型、双突变体和四突变体二氢叶酸还原酶具有亚纳摩尔效力。

产品描述

WR-99210 is a potent inhibitor of Plasmodium falciparum dihydrofolate reductase (pfDHFR), which is a major malarial drug target. It has subnanomolar potency for the wild type, double mutant and quadruple mutant dihydrofolate reductases.

体外活性

When tested in vitro against drug-resistant clones of P. falciparum, PS-15 was more active than proguanil, and the putative metabolite, WR99210, was more active than the proguanil metabolite cycloguanil[1].

体内活性

QR992210 is more active as well as less toxic than proguanil when administered orally to mice infected with P. berghei. When administered orally to Aotus monkeys infected with multidrug-resistant P. falciparum, PS-15 was more active than either proguanil or WR99210[1].

Cas No.

30711-93-4

分子式

C14H19Cl4N5O2

分子量

431.14

别名

6,6-Dimethyl-1-[3-(2,4,5-trichlorophenoxy)propoxy]-1,6-dihydro-1,3,5-triazine-2,4-diamine;WR99210 hydrochloride(47326-86-3 free base);WR-99210

储存和溶解度

DMSO:55 mg/ml (127.57 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
 
 
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