Description
GNE-495 is a potent and selective MAP4K4 inhibitor with an IC50 of 3.7 nM.
Product information
CAS Number: 1449277-10-4
Molecular Weight: 405.42
Formula: C22H20FN5O2
Chemical Name: 8-amino-N-(1-cyclopropanecarbonylazetidin-3-yl)-2-(3-fluorophenyl)-1,7-naphthyridine-5-carboxamide
Smiles: NC1N=CC(=C2C=CC(=NC2=1)C1=CC(F)=CC=C1)C(=O)NC1CN(C1)C(=O)C1CC1
InChiKey: FYXCIBJXJYBWPX-UHFFFAOYSA-N
InChi: InChI=1S/C22H20FN5O2/c23-14-3-1-2-13(8-14)18-7-6-16-17(9-25-20(24)19(16)27-18)21(29)26-15-10-28(11-15)22(30)12-4-5-12/h1-3,6-9,12,15H,4-5,10-11H2,(H2,24,25)(H,26,29)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 2.17 mg/mL (5.35 mM; Need ultrasonic). H2O : 1 mg/mL (2.47 mM; ultrasonic and warming and heat to 80°C).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
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.
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%).
Products are for research use only. Not for human use.
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