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GNE-495 is a potent and selective MAP4K4 Inhibitor with efficacy in retinal angiogenesis. GNE-495 showed excellent potency and good PK and was used to demonstrate in vivo efficacy in a retinal angiogenesis model recapitulating effects that were observed in the inducible Map4k4 knockout mice. GNE-495 is administered intraperitoneally to neonatal mouse pups at high doses: 25 and 50 mg/kg.
| Molecular Weight | 405.42 |
| Formula | C22H20FN5O2 |
| CAS Number | 1449277-10-4 |
| Solubility (25°C) | DMSO 2 mg/mL (Need ultrasonic) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related MAPKAPK2/MAP3K/MAP4K Products |
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ASK1-IN-1 is a novel CNS-penetrant apoptosis signal-regulating kinase 1 (ASK1) inhibitor with good potency (cell IC50 = 138 nM), low clearance (rat Cl/Clu = 0.36/6.7 L h-1 kg-1) and good CNS penetration (rat K p,uu = 0.38). |
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| MSC 2032964A
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| INS018 055
INS018 055 is a TNIK and MAP4K4 inhibitor with IC50 values of 12-120 nM, respectively. INS018 055 exhibits anti-fibrotic activity across different organs in vivo through oral, inhaled or topical administration. INS018 055 possesses anti-inflammatory effects in addition to its anti-fibrotic profile, validated in multiple in vivo studies. |
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