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