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. In Vivo: p38 MAPK-IN-1 (Compound 4; 1 mg/kg for iv and 10 mg/kg for po) has a t_1/2 of 7.4 hours and CL of 2.7 mL/min/kg for iv, and a C_max of 5.3 μM for po in male wistar rats^[1].
p38 MAPK-IN-1 dose-dependently inhibits TNFα production with an ED₅₀ of 0.5 mg/kg^[1].