• 提示：详情请下载说明书。

• 产品描述： SB-649868 is a potent and selective orally active orexin (OX) 1 and OX2 receptor antagonist (pKi =9.4 and 9.5 at the OX1 and OX2 receptor, respectively).

• 靶点： pKi: 9.4 (OX1), 9.5 (OX2);OXReceptor

• 体外研究：
  SB-649868 is identified as one the most in vitro potent dual OX1 and OX2 receptor antagonist known at that time (pKi=9.4 and 9.5 at the OX1 and OX2 receptor, respectively) . SB-649868 antagonizes orexin-A-induced inositol 1 phosphate (IP1) accumulation with the following pKB value (OX1=9.67; OX2=9.64). SB-649868 displaces the [3H]ACT-078573 receptor binding with the following pKi values: OX1=9.27; OX2=8.91. Increasing concentrations of SB-649868 (0.3 nM-30 nM) induces a rightward shift of the orexin-A CRCs with a depression of the agonist efficacy suggesting a clear non-surmountable behavior. The calculated apparent pKb values are 9.67±0.03 and 9.64±0.07 for OX1 and OX2.

• 参考文献：
  1. Di Fabio R, et al. Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2receptor antagonist useful for treatment of sleep disorders. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5562-7. 2. Faedo S, et al. Functional and binding kinetic studies make a distinction between OX1 and OX2 orexin receptorantagonists. Eur J Pharmacol. 2012 Oct 5;692(1-3):1-9.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.094 ml	10.47 ml	20.94 ml
  5 mM	0.419 ml	2.094 ml	4.188 ml
  10 mM	0.209 ml	1.047 ml	2.094 ml
  50 mM	0.042 ml	0.209 ml	0.419 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 *