p38 MAPK-IN-4

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

p38 MAPK-IN-4 是一种有效的选择性 p38 MAPK 抑制剂，对 p38α 的 IC50 为 68 nM。

p38 MAPK-IN-4 is a potent and selective inhibitor of p38 MAPK with IC50 of 68 nM for p38α, inhibits LPS-induced TNFα release in THP-1 cells with IC50 of 187 nM; displays no signigicant activity against a panel of 54 tyrosine kinases and serine/threonine kinases; dose-dependently inhibits TNFα production with an ED50 of 0.5 mg/kg in rat-LPS induced TNFα model, dose-dependently inhibits arthritis progression with ED50 <1 mg/kg, demonstrates a superior efficacy of 4 versus other clinically tested reference compounds like BIRB-796 and VX-745.

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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. p38 MAPK-IN-1 dose-dependently inhibits TNFα production with an ED50 of 0.5 mg/kg. 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 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.

p38alpha-IN-4 | p38alpha IN 4 | p38alphaIN4 | p38alpha inhibitor 4 | p38alpha-inhibitor-4 | p38 MAP Kinase Inhibitor XI |

MAPK/ERK Signaling

p38 MAPK

p38 MAPK

Cancer

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1006378-90-0

349.3534

C21H15F2N2O

>98% (HPLC)

10 mM in DMSO

[O-][N+]1=C(C2=CC=CC=C2C)C3=NC=CC(C4=CC=C(F)C=C4F)=C3C=C1

1,7-Naphthyridine, 4-(2,4-difluorophenyl)-8-(2-methylphenyl)-, 7-oxide

(-20℃)

With Ice Pack

≥ 2 years