產品描述: | SD 0006 (SD-06) is an orally active, selective, ATP-competitive and potent diaryl pyrazole inhibitor of p38α MAP kinase, with an IC50 of 110 nM for p38α |
靶點: |
IC50: 110 nM (p38 MAPK);p38MAPK;Autophagy |
體外研究: |
SD 0006 clearly inhibits p38α as shown by the dose-dependent inhibition of phosphorylation of its endogenous Hsp27 substrate |
體內研究: |
SD 0006 (0-30 mg/kg) may be an effective alternative to steroids and biologics for RA therapy. SD0006 (3.75, 7.5 and 15 mg/kg; p.o.; b.i.d.) is highly effective in attenuating SCW-induced inflammation as shown by the dose-dependent inhibition of paw swelling. Animal Model: 8- to 12-week-old DBA/1 mice. Dosage: 3.75, 7.5 and 15 mg/kg. Administration: Orally twice daily. Result: Inhibited the transcription of several inflammatory mediators to prevent joint swelling and bone destruction and to preserve bone density. |
參考文獻: |
1. Burnette BL, et al. SD0006: a potent, selective and orally available inhibitor of p38 kinase. Pharmacology. 2009;84(1):42-60. 2. Walker JK, et al. Identification of SD-0006, a potent diaryl pyrazole inhibitor of p38 MAP kinase. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2634-8. |
溶解性: |
Soluble in DMSO |
保存條件: |
-20℃ |
配置溶液濃度參考: |
|
1mg |
5mg |
10mg |
1 mM |
2.513 ml |
12.567 ml |
25.135 ml |
5 mM |
0.503 ml |
2.513 ml |
5.027 ml |
10 mM |
0.251 ml |
1.257 ml |
2.513 ml |
50 mM |
0.05 ml |
0.251 ml |
0.503 ml |
|
注意: |
部分產品我司僅能提供部分信息,我司不保證所提供信息的權威性,僅供客戶參考交流研究之用。 |