| Identification | Back 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 Properties | Back 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 Information | Back 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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| Company Name: |
SPIRO PHARMA
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| Tel: |
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| Website: |
www.spiropharma.com.cn |
| Company Name: |
BOC Sciences
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16314854226 |
| Website: |
www.bocsci.com |
| Company Name: |
Musechem
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+1-800-259-7612 |
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www.musechem.com |
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