p38 MAPK-IN-1 (Compound 4) is a novel potent and selective inhibitor of p38 MAPK with IC 50 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 . p38 MAPK-IN-1 dose-dependently inhibits TNFα production with an ED 50 of 0.5 mg/kg . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male wistar rats Dosage: 10 mg/kg for po and 1 mg/kg for iv (Pharmacokinetic Analysis) Administration: Po and iv Result: Had 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.