• 提示：详情请下载说明书。

• 产品描述： R1487 Hydrochloride is a highly potent and selective p38α inhibitor, with Kd values of 0.2 nM and 29 nM for p38α and p38β, respectively

• 靶点： p38α:0.2 nM (Kd);p38β:29 nM (Kd);p38MAPK;Autophagy

• 体外研究：
  R1487 Hydrochloride exhibits IC50 values of 10 nM for p38α inhibition and 200 nM for the inhibition of TNFα induced production of IL-1β. R1487 (Compounds 2a) inhibits production of TNFα by human monocytic cells (THP-1) and inhibits production of IL-1β in human whole blood (HWB) induced by LPS

• 体内研究：
  R1487 (Compounds 2a, orally) demonstrates significant dose-dependent inhibition of serum TNFα and IL-1β. Oral bioavailability of 10 mg/kg R1487 (Compounds 2a) in monkey, rat, and dog was 51.6%, 29.3%, 10.3%, respectively

• 参考文献：
  1. Goldstein DM, Soth M, Gabriel T,et al.Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally bioavailable and highly selective inhibitors of p38α mitogen-activated protein kinase[J].J Med Chem. 2011 Apr 14;54(7):2255-65.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.354 ml	11.769 ml	23.539 ml
  5 mM	0.471 ml	2.354 ml	4.708 ml
  10 mM	0.235 ml	1.177 ml	2.354 ml
  50 mM	0.047 ml	0.235 ml	0.471 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。

输入产品批号：

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *