产品描述: | 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. |
靶点: |
p38 MAPK:68 nM (IC50);p38MAPK |
体内研究: |
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. |
参考文献: |
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. |
溶解性: |
soluble in DMSO |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.862 ml |
14.312 ml |
28.624 ml |
5 mM |
0.572 ml |
2.862 ml |
5.725 ml |
10 mM |
0.286 ml |
1.431 ml |
2.862 ml |
50 mM |
0.057 ml |
0.286 ml |
0.572 ml |
|
注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |