DSM265
规格
| Cas Number | 1282041-94-4(DMSO) |
| 规格或纯度 | 10mM in DMSO |
| 包装 | 1ml |
产品信息
| 品牌 | 阿拉丁 |
| 浓度 | 10mM in DMSO |
| 过滤标签 | Dihydroorotate Dehydrogenase,Parasite,Metabolic Enzyme/Protease,Anti-infection,Compound libraries |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | DSM265 是恶性疟原虫二氢烟酸脱氢酶（Pf DHODH）的长效抑制剂，IC 50 为 8.9 nM。DSM265 还能抑制 Pf 3D7 寄生虫的生长，其 EC 50 为 4.3 nM。 |
| 英文描述 |
DSM265 is a long-duration inhibitor of P. falciparum dihydroorotate dehydrogenase ( Pf DHODH ) with an IC 50 of 8.9 nM. DSM265 can also inhibit the growth of Pf 3D7 parasites with an EC 50 of 4.3 nM In Vivo DSM265 (0.5 to 75 mg/kg; Oral administration; twice daily; for 4 days; NOD- scid IL-2Rγ (NSG) mice) has potent in vivo antimalarial activity with 90% effective dose ( ED 90 ) of 3 mg/kg per day (1.5 mg/kg twice daily). The maximum rate of parasite killing occurred at and above a dose of 13 mg/kg per day (6.4 mg/kg twice daily). DSM265 has moderate terminal elimination half-life (t 1/2 ) of 2-4 hours for mice (0.5 to 75 mg/kg, oral). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: NOD- scid IL-2Rγ (NSG) mice (23-36 g)Dosage: 0.5 to 75 mg/kg Administration: Oral administration; twice daily; for 4 days Result: Had potent antimalarial activity with 90% effective dose ( ED 90 ) of 3 mg/kg per day (1.5 mg/kg twice daily). IC50& Target:IC50: 8.9 nM ( Pf DHODH), EC50: 4.3 nM ( P. falciparum 3D7 parasites) |