| 產(chǎn)品描述： | VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β |
| 靶點(diǎn)： |
p38α MAPK;p38MAPK;Autophagy |
| 體內(nèi)研究： |
The half-life of VX-702 is 16 to 20 hours, with a median clearance of 3.75 L/h and a volume of distribution of 73 L/kg. Both AUC and Cmax values are dose proportional for VX-702, which is predominantly cleared renally. VX-702 (at a dose of 0.1 mg/kg twice daily) has an equivalent effect as that of methotrexate (0.1 mg/kg). In addition, VX-702 (5 mg/kg twice daily) also has an equivalent effect as prednisolone (10 mg/kg once daily), as measured by percentage inhibition of wrist joint erosion and inflammation score. |
| 參考文獻(xiàn)： |
1. Kuliopulos A, et al. Effect of selective inhibition of the p38 MAP kinase pathway on platelet aggregation. Thromb Haemost, 2004, 92(6), 1387-1393. 2. Braddock M, IDDB Meeting Report, 2005, March 14-15. 3. Gill A, IDDB Meeing Report, 2002, March 06-08. 4. Naka K, et al. Dipeptide species regulate p38MAPK-Smad3 signalling to maintain chronic myelogenous leukaemia stem cells. Nat Commun. 2015 Aug 20;6:8039. |
| 溶解性： |
DMSO : ≥ 42 mg/mL (103.88 mM) |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.473 ml |
12.366 ml |
24.733 ml |
| 5 mM |
0.495 ml |
2.473 ml |
4.947 ml |
| 10 mM |
0.247 ml |
1.237 ml |
2.473 ml |
| 50 mM |
0.049 ml |
0.247 ml |
0.495 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)營許可證（不帶存儲(chǔ)）
營業(yè)執(zhí)照(三證合一)
北京