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GNE-495

GNE-495 是有效选择性的MAP4K4抑制剂(IC50=3.7 nM)。

CAS号

1449277-10-4

分子式

C22H20FN5O2

主要靶点

MAPK

仅限科研使用

Cat No : CM05024

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Synonyms

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  • CAS No.: 1449277-10-4

    GNE-495
    CAS#: 1449277-10-4

产品信息

GNE-495 is a potent and specific MAP4K4 inhibitor (IC50: 3.7 nM).

CAS号 1449277-10-4
分子式 C22H20FN5O2
主要靶点 MAPK
主要通路 MAPK信号通路
分子量 405.42
纯度 98.23%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名

靶点活性

MAP4K4:3.7nM

体内活性

GNE-495 is administered intraperitoneally to neonatal mouse pups at high doses: 25 and 50 mg/kg. GNE-495 shows excellent potency and good PK in vivo profile in all species tested, with low clearances, moderate terminal half-lives, and reasonable oral exposure levels (F=37-47%).

体外活性

GNE-495 has efficacy in retinal angiogenesis. GNE-495 shows the best balance of MAP4K4 inhibition, permeability, microsomal stability, and cellular potency.

溶解度

DMSO:2 mg/mL (4.93 mM),Sonification is recommended.

参考文献

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.

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