中文名称:

CS-2117

中文同义词:

P38MAPK抑制剂(P38 MAPK-IN-1)

英文名称:

p38 MAPK-IN-1

英文同义词:

p38 MAPK-IN-1;CS-2117;p38 MAPK-IN-4;1,7-Naphthyridine, 4-(2,4-difluorophenyl)-8-(2-methylphenyl)-, 7-oxide

CAS号:

1006378-90-0

分子式:

C21H14F2N2O

分子量:

348.35

EINECS号:

相关类别:

细胞生物学试剂

Mol文件:

1006378-90-0.mol

沸点 

527.0±50.0 °C(Predicted)

密度 

1.27±0.1 g/cm3(Predicted)

酸度系数(pKa)

0.26±0.40(Predicted)

生物活性

p38 MAPK-IN-1 (Compound 4) 是 p38 MAPK 新型高效选择性抑制剂, IC50 值 68 nM。p38 MAPK-IN-1 显示持续水平，低清除率和良好的生物利用度。

靶点

p38 MAPK 68 nM (IC 50 )

p38 MAPK 68 nM (IC 50 )

体内研究

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. 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.

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.