ChemicalBook--->CAS DataBase List--->1310455-86-7

1310455-86-7

1310455-86-7 Structure

1310455-86-7 Structure
IdentificationBack Directory
[Name]

GNF179 Metabolite
[CAS]

1310455-86-7
[Synonyms]

EOS-60885
GNF179 Metabolite
2-(4-fluorophenyl)-8,8-dimethyl-6,7-dihydro-5H-imidazo[1,2-a]pyrazine
2-(4-fluorophenyl)-8,8-dimethyl-5,6,7,8-tetrahydroimidazo[1,2-a]pyrazine
Imidazo[1,2-a]pyrazine, 2-(4-fluorophenyl)-5,6,7,8-tetrahydro-8,8-dimethyl-
[Molecular Formula]

C14H16FN3
[MDL Number]

MFCD22690265
[MOL File]

1310455-86-7.mol
[Molecular Weight]

245.3
Chemical PropertiesBack Directory
[Boiling point ]

428.6±40.0 °C(Predicted)
[density ]

1.23±0.1 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

Soluble in DMSO
[form ]

Powder
[pka]

8.43±0.40(Predicted)
Hazard InformationBack Directory
[Uses]

GNF179 metabolite is the metabolite of GNF179, which 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: 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.
[storage]

Store at -20°C
[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. DOI:10.1126/science.1211936
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