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

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

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

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%).

1449277-10-4

C22H20FN5O2

405.42

DMSO:2 mg/mL (4.93 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years