產(chǎn)品描述: | GNE-495 is a potent and selective MAP4K4 inhibitor with an IC50 of 3.7 nM. |
靶點(diǎn): |
MAP4K4:3.7 nM (IC50);MAPK |
體外研究: |
GNE-495 is a potent and selective MAP4K4 inhibitor with efficacy in retinal angiogenesis. GNE-495 shows the best balance of MAP4K4 inhibition, permeability, microsomal stability, and cellular potency |
體內(nèi)研究: |
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%) |
參考文獻(xiàn): |
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. |
溶解性: |
soluble in DMSO |
保存條件: |
-20℃ |
配置溶液濃度參考: |
|
1mg |
5mg |
10mg |
1 mM |
2.467 ml |
12.333 ml |
24.665 ml |
5 mM |
0.493 ml |
2.467 ml |
4.933 ml |
10 mM |
0.247 ml |
1.233 ml |
2.467 ml |
50 mM |
0.049 ml |
0.247 ml |
0.493 ml |
|
注意: |
部分產(chǎn)品我司僅能提供部分信息,我司不保證所提供信息的權(quán)威性,僅供客戶參考交流研究之用。 |