GNE-495 |
Catalog No.GC18257 |
GNE-495 is an orally bioavailable, potent, and selective MAP4K4 inhibitor (IC50 = 3.7 nM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1449277-10-4
Sample solution is provided at 25 µL, 10mM.
GNE-495 is a potent and selective MAP4K4 inhibitor with an IC50 of 3.7 nM.
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[1].
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].
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.
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