计算溶液所需的质量、体积或浓度。
提供 ≥99% 纯度,适用于对基线干扰要求严格的色谱和分析工作流程。
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在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
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 . 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