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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related MAPKAPK2/MAP3K/MAP4K Products |
|---|
| MAP4K4-IN-3
MAP4K4-IN-3 is a potent and selective MAP4K4 inhibitor with an IC50 of 14.9 nM in kinase assay, and an IC50 of 470 nM in cell assay. |
| PROTAC MLKL Degrader-1
PROTAC MLKL Degrader-1 is a PROTAC degrader of MLKL, with a Dmax ＞90%. |
| HPK1-IN-37
HPK1-IN-37 is an inhibitor of HPK1 (IC50=3.7 nM). |
| GNE-6893
GNE-6893 is a potent and orally active HPK1 inhibitor. |
| HPK1-IN-39
HPK1-IN-39 is a selective HPK1 Inhibitor (IC50: 29 nM). |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
