1006378-90-0
中文名稱
CS-2117
英文名稱
p38 MAPK-IN-1
CAS
1006378-90-0
分子式
C21H14F2N2O
分子量
348.35
MOL 文件
1006378-90-0.mol
更新日期
2023/03/20 15:41:27
1006378-90-0 結(jié)構(gòu)式
基本信息
中文別名
P38MAPK抑制劑(P38 MAPK-IN-1) 英文別名
CS-2117p38 MAPK-IN-1
p38 MAPK-IN-4
1,7-Naphthyridine, 4-(2,4-difluorophenyl)-8-(2-methylphenyl)-, 7-oxide
物理化學(xué)性質(zhì)
沸點527.0±50.0 °C(Predicted)
密度1.27±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度DMSO: 8.33 mg/mL (23.84 mM)
酸度系數(shù)(pKa)0.26±0.40(Predicted)
形態(tài)Solid
顏色Off-white to yellow
常見問題列表
生物活性
p38 MAPK-IN-1 (Compound 4) 是 p38 MAPK 新型高效選擇性抑制劑, IC50 值 68 nM。p38 MAPK-IN-1 顯示持續(xù)水平，低清除率和良好的生物利用度。靶點
|
p38 MAPK 68 nM (IC 50 ) |
體內(nèi)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. |