| 產(chǎn)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. |
| 靶點(diǎn)： |
p38 MAPK:68 nM (IC50);p38MAPK |
| 體內(nèi)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. |
| 參考文獻(xiàn)： |
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 |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
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： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
上海工商
危險(xiǎn)品化學(xué)品經(jīng)營(yíng)許可證（不帶存儲(chǔ)）
營(yíng)業(yè)執(zhí)照(三證合一)
北京