| Identification | Back Directory | [Name]
GNE-495 | [CAS]
1449277-10-4 | [Synonyms]
GNE-495
GNE-495;GNE 495;GNE495
8-Amino-N-[1-(cyclopropylcarbonyl)-3-azetidinyl]-2-(3-fluorophenyl)-1,7-naphthyridine-5-carboxamide
8-amino-N-(1-(cyclopropanecarbonyl)azetidin-3-yl)-2-(3-fluorophenyl)-1,7-naphthyridine-5-carboxamide
1,7-Naphthyridine-5-carboxamide, 8-amino-N-[1-(cyclopropylcarbonyl)-3-azetidinyl]-2-(3-fluorophenyl)- | [Molecular Formula]
C22H20FN5O2 | [MDL Number]
MFCD30489735 | [MOL File]
1449277-10-4.mol | [Molecular Weight]
405.42 |
| Chemical Properties | Back Directory | [Boiling point ]
734.5±60.0 °C(Predicted) | [density ]
1.45±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:3.59(Max Conc. mg/mL);8.85(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:7):0.125(Max Conc. mg/mL);0.31(Max Conc. mM)
DMF:5.0(Max Conc. mg/mL);12.33(Max Conc. mM)
Water:1.0(Max Conc. mg/mL);2.47(Max Conc. mM) | [form ]
A crystalline solid | [pka]
11.60±0.20(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
GNE-495 is a potent and selective MAP4K4 inhibitor with an IC50 of 3.7 nM. | [in vivo]
GNE-495 is administered intraperitoneally to neonatal mouse pups at high doses: 25 and 50 mg/kg. GNE-495 shows good in vivo profile in all species tested, with low clearances, moderate terminal half-lives, and reasonable oral exposure levels (F=37-47%)[1]. | [IC 50]
MAP4K4: 3.7 nM (IC50) | [References]
[1] Ndubaku CO et al. Structure-Based Design of GNE-495, a Potent and Selective MAP4K4 Inhibitor with Efficacy in Retinal Angiogenesis. ACS Med Chem Lett. 2015 Jun 29;6(8):913-8. DOI:10.1021/acsmedchemlett.5b00174 |
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| Company Name: |
Musechem
|
| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
|