| Bioactivity | 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 t1/2 of 7.4 hours and CL of 2.7 mL/min/kg for iv, and a Cmax 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]. Animal Model: | ||||||||||||
| Name | p38 MAPK-IN-1 | ||||||||||||
| CAS | 1006378-90-0 | ||||||||||||
| Formula | C21H15F2N2O | ||||||||||||
| Molar Mass | 349.35 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Lumeras W, et al. 1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase. J Med Chem. 2011 Nov 24;54(22):7899-910. |
p38 MAPK-IN-1
CAS: 1006378-90-0 F: C21H15F2N2O W: 349.35
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
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