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• 产品描述： Almorexant (ACT 078573) hydrochloride is an orally active, potent and competitive dual orexin receptor antagonist, with Kd values of 1.3 nM (OX1) and 0.17 nM (OX2), respectively. Almorexant hydrochloride reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant hydrochloride totally blocked the intracellular Ca2+ signal pathway. Almorexant hydrochloride stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis

• 靶点： human OX2R:0.17 nM (Kd);human OX1R:1.3 nM (Kd);Caspase-3 ;OXReceptor

• 体内研究：
  Almorexant hydrochloride (1.8 μmol/kg, 100 μL; IP, daily) reduces the volume of tumors. Almorexant hydrochloride (300 mg/kg, PO, once) can help rats to be fully capable of spatial and avoidance learning. Almorexant hydrochloride (30-300 mg/kg) dose-dependently increases rapid eye movement (REM) and non-REM (NREM) sleep and decreases wakefulness apparently without inducing either cataplexy18 or deficits in next-day performance.

• 参考文献：
  1. Dayot S, et al. In vitro, in vivo and ex vivo demonstration of the antitumoral role of hypocretin-1/orexin-A and almorexant in pancreatic ductal adenocarcinoma. Oncotarget. 2018 Jan 9;9(6):6952-6967. 2. Malherbe P, et al. Biochemical and electrophysiological characterization of almorexant, a dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist: comparison with selective OX1 and OX2 antagonists. Mol Pharmacol. 2009 Sep;76(3):618-31. 3. Black SW, et al. Almorexant promotes sleep and exacerbates cataplexy in a murine model of narcolepsy. Sleep. 2013 Mar 1;36(3):325-36. 4. Dietrich H, et al. Intact learning and memory in rats following treatment with the dual orexin receptor antagonist almorexant. Psychopharmacology (Berl). 2010 Oct;212(2):145-54.

• 溶解性： DMSO  :  ≥  46  mg/mL  (83.79  mM)    H2O  :  <  0.1  mg/mL  (ultrasonic;warming;heat  to  60°C)  (insoluble)

• 保存条件： RT

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.951 ml	9.755 ml	19.51 ml
  5 mM	0.39 ml	1.951 ml	3.902 ml
  10 mM	0.195 ml	0.975 ml	1.951 ml
  50 mM	0.039 ml	0.195 ml	0.39 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 *