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• 产品描述： MK-1064 is a selective and orally active OX2R antagonist (Ki: 0.5 nM, IC50: 18 nM). MK-1064 promotes sleep in vivo. MK-1064 can be used in the research of insomnia

• 靶点： OX2 Receptor:18 nM (IC50);OX1 Receptor:1789 nM (IC50);OX2 Receptor:0.5 nM (Ki);OX1 Receptor;1584 nM (Ki);OXReceptor

• 体内研究：
  MK-1064 (30 mg/kg, oral administration) promotes sleep in rodents selectively through OX2R in Wild-type mice. MK-1064 (30 mg/kg, oral administration, 5 days) reverses the struggle behavior induced by CNO pre-treatment in rats. MK-1064 (1-5 mg/kg, intravenous injection/oral administration) shows moderate oral bioavailability and clearance in rat, dog, and rhesus monkey. Animal Model: Wild-type and OX2R knockout mice Dosage: 30 mg/kg Administration: Oral administration Result: Displayed active wake reduction accompanied by significant increases in SWS (slow-wave sleep) and REM (rapid eye movement) at time points up to 3.5 hours following treatment. Animal Model: Rat, dog, and rhesus monkey (Pharmacokinetics assay) Dosage: 1, 2, 3, 5 mg/kg Administration: Oral administration (P.O.), intravenous injection (I.V.) Result: Pharmacokinetics profile of MK-1064.

• 参考文献：
  1. Roecker AJ et al. Discovery of 5''-chloro-N-[(5,6-dimethoxypyridin-2-yl)methyl]-2,2':5',3''-terpyridine-3'-carboxamide (MK-1064): a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia. ChemMedChem. 2014 Feb;9(2):311-22. 2. Gotter AL et al. Orexin 2 Receptor Antagonism is Sufficient to Promote NREM and REM Sleep from Mouse to Man. Sci Rep. 2016 Jun 3;6:27147. 3. Laura A Grafe, et al. Orexin 2 receptor regulation of the hypothalamic-pituitary-adrenal (HPA) response to acute and repeated stress. Neuroscience. 2017 Apr 21;348:313-323.

• 溶解性： soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.165 ml	10.825 ml	21.65 ml
  5 mM	0.433 ml	2.165 ml	4.33 ml
  10 mM	0.216 ml	1.082 ml	2.165 ml
  50 mM	0.043 ml	0.216 ml	0.433 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 *