1261114-01-5

1261114-01-5 structure

Name: GNF179
Chemical Name: gnf179
CAS Number: 1261114-01-5
Molecular Formula: C₂₂H₂₃ClFN₅O
Molecular Weight: 427.90200
Catalog: Signaling Pathways Anti-infection Parasite
Create Date: 2016-05-02 22:39:26
Modify Date: 2024-01-30 14:11:29
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.

Name	gnf179

Description	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.
Related Catalog	Signaling Pathways >> Anti-infection >> Parasite Research Areas >> Infection
References	[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.