| Description | WR99210 hydrochloride 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. |
| In vitro | 在体外针对抗药性P. falciparum克隆进行测试时，PS-15的活性高于proguanil，而其假定的代谢产物WR99210的活性则高于proguanil的代谢产物cycloguanil[1]。 |
| In vivo | QR992210在经口给予感染了P. berghei的小鼠时，表现出比proguanil更高的活性和更低的毒性。经口给予感染了多重耐药P. falciparum的Aotus猴时，PS-15比proguanil或WR99210[1]的活性更强。 |
| Synonyms | WR99210 hydrochloride(47326-86-3 free base), 6,6-Dimethyl-1-[3-(2,4,5-trichlorophenoxy)propoxy]-1,6-dihydro-1,3,5-triazine-2,4-diamine |
| molecular weight | 431.14 |
| Molecular formula | C14H19Cl4N5O2 |
| CAS | 30711-93-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 55 mg/ml (127.57 mM) |
| References | 1. Canfield C J , Milhous W K , Ager A L , et al. PS-15: a potent, orally active antimalarial from a new class of folic acid antagonists.[J]. American Journal of Tropical Medicine & Hygiene, 1993, 49(1):121. |
WR99210 hydrochloride(47326-86-3 free base)
CAS No.: 30711-93-4
WR99210 hydrochloride is a potent inhibitor of Plasmodium falciparum dihydrofolate reductase (pfDHFR), which is a major
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