S84720 |
SD-06 |
MedMol | 97% |
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- 产品描述: 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
- 靶点: IC50: 110 nM (p38 MAPK);p38MAPK;Autophagy
- 体外研究:
SD 0006 clearly inhibits p38α as shown by the dose-dependent inhibition of phosphorylation of its endogenous Hsp27 substrate
- 体内研究:
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.
- 参考文献:
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
- 保存条件: -20℃
- 配置溶液浓度参考:
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
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)