GNF179
规格
| Cas Number | 1261114-01-5 |
| 规格或纯度 | ≥99% |
| 纯度 | ≥99% |
| 包装 | 100mg 或 50mg 或 10mg 或 1mg 或 5mg |
产品信息
| 品牌 | 阿拉丁 |
| 溶解性 | DMSO : 100 mg/mL (233.70 mM; Need ultrasonic) |
| 过滤标签 | Parasite,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 | GNF179 是一种优化的 8,8-二甲基咪唑哌嗪类似物，具有抗疟效力（对耐多药菌株 W2 的 IC 50 为 4.8 nM）。GNF179 具有口服活性。 |
| 英文描述 |
GNF179 is an optimized 8,8-dimethyl imidazolopiperazine analog that exhibits antimalarial potency ( IC 50 of 4.8 nM against the multidrug resistant strain W2). GNF179 is orally active In Vitro GNF179 does not rapidly inhibit parasite protein biosynthesis nor is it likely to target parasite cytochrome bc1, which has been validated as a hepatic stage target for Atovaquone (HY-13832). GNF179 may act against sporozoites instead of hepatic stages. GNF179 (5-100 nM; 48 h) shows high inhibition of gametocyte sexual life cycle progression in the mosquito as it abolished oocyst formation at 5 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo GNF179 (15 mg/kg; p.o.; single dose) shows antimalarial activity in rodent malaria model . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Naïve Balb/C mice infected with P. berghei Dosage: 15 mg/kg Administration: Oral, single dose Result: Protected against an infectious P. berghei sporozoite. Animal Model: Naïve Balb/C mice Dosage: 3 or 20 mg/kg Administration: IV or PO (Pharmacokinetic Analysis) Result: Pharmacokinetics of GNF179 in naïve Balb/C mice . Dose AUC (0-∞) (hrs*µM) AUC/dose t 1/2 (hrs) MRT (hrs) CL (ml/min/kg) V ss (L/kg) C 0 or C max (µM) F (%) 3 mg/kg i.v. 8.88 3.0 8.9 9.0 22 11.8 6.1 nd 20 mg/kg p.o. 20.70 1.0 8.4 nd nd nd 1.2 58 AUC, Area Under the Curve; T 1/2 , half life; CL, clearance; V SS , steady-state volume of distribution; C 0 , initial concentration; C max maximum concentration; F, fraction of dose absorbed; hrs, hours; nd, not determined. Form:Solid IC50& Target:Plasmodium |