WR99210
规格
Cas Number | 47326-86-3 |
规格或纯度 | ≥98% |
纯度 | ≥98% |
包装 | 50mg 或 10mg |
产品信息
品牌 | 阿拉丁 |
溶解性 | DMSO : 5 mg/mL (12.67 mM; Need ultrasonic) |
过滤标签 | Parasite,Dihydrofolate reductase (DHFR),Metabolic Enzyme/Protease,Anti-infection |
储存温度 | -20°C储存 |
运输条件 | 超低温冰袋运输 |
生化和生理学机理 | WR99210 是一种口服活性低毒性二氢叶酸还原酶 (DHFR) 抑制剂(IC 50 <0.075 nM)。WR99210 显示出良好的抗寄生虫活性,对恶性疟原虫和恶性疟原虫菌株(包括抗嘧啶胺(HY-18062)菌株)有效。 |
英文描述 |
WR99210 is an orally active and low-toxicity dihydrofolate reductase (DHFR) inhibitor ( IC 50 <0.075 nM). WR99210 shows good antiparasitic activity and is effective against P. falciparum and P. falciparum strains (including Pyrimethamine (HY-18062)-resistant P. falciparum strains) as well as T. gondii In Vitro WR99210 (0-100 nM; 92 h) is highly effective against T. gondii tachyzoites in tissue culture. WR99210 (0-100 nM; 92 h) shows low cytotoxicity to human foreskin fibroblasts. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Human foreskin fibroblasts ( T. gondii -infected) Concentration: 0-100 nM Incubation Time: 92 h Result: Showed marked inhibition of T. gondii , with an IC 50 value of approximately 50 nM. Cell Cytotoxicity AssayCell Line: Human foreskin fibroblasts Concentration: 0-100 nM Incubation Time: 92 h Result: Lacked of toxicity for fibroblasts. In Vivo WR99210 (1.25 mg/kg; i.p.; single daily for 5 days) is highly effective against T. gondii tachyzoites in a mouse model . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male mice ( T. gondii -infected) . Dosage: 1.25 mg/kg Administration: Intraperitoneal injection; single daily for 5 days. Result: Exhibited intraperitoneal parasite numbers were 2 logs less in mice on the day 5. Form:Solid IC50& Target:IC50: <0.075 nM (DHFR) |