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GNE-495 is a potent and specific inhibitor of MAP4K4 with an IC50 of 3.7 nM.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $66 | In Stock | |
5 mg | $97 | In Stock | |
10 mg | $148 | In Stock |
Description | GNE-495 is a potent and specific inhibitor of MAP4K4 with an IC50 of 3.7 nM. |
Targets&IC50 | MAP4K4:3.7nM |
In vitro | GNE-495 has 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 at high doses (25 and 50 mg/kg) intraperitoneally to neonatal mice. This compound demonstrates superior potency and favorable pharmacokinetic (PK) profiles across all tested species, characterized by low clearance rates, moderate terminal half-lives, and acceptable levels of oral bioavailability (F=37-47%). |
Molecular Weight | 405.42 |
Formula | C22H20FN5O2 |
Cas No. | 1449277-10-4 |
Smiles | Nc1ncc(C(=O)NC2CN(C2)C(=O)C2CC2)c2ccc(nc12)-c1cccc(F)c1 |
Relative Density. | 1.45 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||
Solubility Information | DMSO: 2 mg/mL (4.93 mM), Sonication is recommended. | ||||||||||
Solution Preparation Table | |||||||||||
DMSO
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