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• 产品描述： IPSU is a selective, orally available and brain penetrant OX2R antagonist with a pKi of 7.85.

• 靶点： pKi: 7.85 (OX2R), 6.29 (OX1R);OXReceptor

• 体外研究：
  Orexin receptor antagonists represent attractive targets for the development of drugs for the treatment of insomnia. IPSU binds rapidly and reaches equilibrium very quickly in binding and/or functional assays

• 体内研究：
  IPSU has low blood clearance, shows high maximal blood exposure and AUC after oral dosing. It exhibits an acceptable absolute oral bioavailability and a brain/blood concentration ratio that indicated favorable brain penetration. IPSU increases sleep when dosed during the mouse active phase (lights off); IPSU induces sleep primarily by increasing NREM sleep. IPSU shows a fast onset of action, with a clear increase in total sleep time during the first hour afterdosing. The effect lasts 4-5 h, after which time the total sleep time per hour is the same as on vehicle day

• 参考文献：
  1. Betschart C, et al. Identification of a novel series of orexin receptor antagonists with a distinct effect on sleeparchitecture for the treatment of insomnia. J Med Chem. 2013 Oct 10;56(19):7590-607. 2. Callander GE, et al. Kinetic properties of 'dual' orexin receptor antagonists at OX1R and OX2R orexin receptors. Front Neurosci. 2013 Dec 3;7:230. 3. Hoyer D, et al. Distinct effects of IPSU and suvorexant on mouse sleep architecture. Front Neurosci. 2013 Dec 10;7:235.

• 溶解性： soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.466 ml	12.331 ml	24.661 ml
  5 mM	0.493 ml	2.466 ml	4.932 ml
  10 mM	0.247 ml	1.233 ml	2.466 ml
  50 mM	0.049 ml	0.247 ml	0.493 ml

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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 *