GNF179 |
| Katalog-Nr.GC36172 |
GNF179 ist ein optimiertes 8,8-Dimethyl-IP-Analogon, das die Potenz (4,8 nM gegen den mehrfach resistenten Stamm W2), die metabolische StabilitÄt in vitro und die orale BioverfÜgbarkeit in vivo aufwies.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1261114-01-5
Sample solution is provided at 25 µL, 10mM.
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GNF179 is an optimized 8,8-dimethyl IP analog that exhibited the potency(4.8 nM against the multidrug resistant strain W2) in vitro metabolic stability and in vivo oral bioavailability.IC50 value: 4.8 nM [1]Target: 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). 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. 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.
[1]. Meister S, et al. Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery. Science. 2011 Dec 9;334(6061):1372-7.
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