p38 MAPK-IN-1 (Compound 4) is a novel potent and selective inhibitor of p38 MAPK with IC50 of 68 nM. p38 MAPK-IN-1 shows sustained levels, low clearance and good bioavailability.
Molecular Weight | 349.35 |
CAS Number | 1006378-90-0 |
Solubility (25°C) | DMSO 8.33 mg/mL |
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.
[1] Joseph M Grimes, et al. p38 MAPK inhibition: A promising therapeutic approach for COVID-19
[2] Ana Cuadrado, et al. Mechanisms and functions of p38 MAPK signalling
[4] Lydia R Coulthard, et al. p38(MAPK): stress responses from molecular mechanisms to therapeutics
[5] Tyler Zarubin, et al. Activation and signaling of the p38 MAP kinase pathway
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