GNF179 是8,8-二甲基 IP 类似物。 它表现出对多药耐药菌株 W2 的效力，具有良好的体外代谢稳定性和体内口服生物相容性。

GNF179 is an optimized 8,8-dimethyl IP analog. It exhibited the potency(4.8 nM against the multidrug resistant strain W2) in vitro metabolic stability and in vivo oral bioavailability.

GNF179 was able to protect against an infectious P. berghei sporozoite challenge with a single oral dose at 15 mg/kg while NITD609 was not. GNF179 reduced Plasmodium berghei parasitemia levels by 99.7% with a single 100 mg/kg oral dose, and prolonged mouse survival by an average of 19 days. Anti-parasitic agent GNF179 exhibits a low clearance (CL=22 ml/min/kg, ~25% of hepatic blood flow in mice), a large volume of distribution (steady-state volume of distribution, Vss=11.8 l/kg), a moderate residence time (MRT=9 hours) and suitable terminal half-life (t1/2=8.9 hours).

1261114-01-5

C22H23ClFN5O

427.9

GNF179

DMSO:120 mg/mL (280.44 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years