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• 产品描述： TCS 1102 is a potent, dual orexin receptor antagonist, with Ki values of 0.2 nM and 3 nM for OX2 and OX1 receptors, respectively. TCS 1102 demonstrates excellent brain peneration and moderate bioavailability in rats

• 靶点： OX1 Receptor：3 nM (Ki)；OX2 Receptor：0.2 nM (Ki);OXReceptor

• 体内研究：
  TCS 1102 (compound 18) (15, 50, 100 mg/kg; i.p; single dose) induces locomotion inhibition in rat in a dose dependent manner. TCS-1102 (10 and 20 mg/kg; i.p.; single dose) decreases fear and anxiety in rats after exposure to footshock. Furthermore, TCS-1102 (10 mg/kg; i.p.; single dose) also shows anxiolytic effects for high responders (HR) rat when tested in the elevated T-maze. PK of TCS 1102 in Rat (100 mg/kg; i.p.; measured at 30 min) Animal Model: Male Sprague–Dawley rats (130-160 g) Dosage: 10 and 20 mg/kg Administration: Intraperitoneal injection; 30 min before received the footshocks Result: Decreased fear and anxiety in rats 14 days after exposure to footshock.

• 参考文献：
  1. Bergman JM, et al. Proline bis-amides as potent dual orexin receptor antagonists. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1425-30. 2. Turku A, et al. Orexin receptor agonist Yan 7874 is a weak agonist of orexin/hypocretin receptors and shows orexin receptor-independent cytotoxicity. PLoS One. 2017 Jun 2;12(6):e0178526. 3. Chen X, et al. Orexins (hypocretins) contribute to fear and avoidance in rats exposed to a single episode of footshocks. Brain Struct Funct. 2013 Aug 18.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.125 ml	10.625 ml	21.25 ml
  5 mM	0.425 ml	2.125 ml	4.25 ml
  10 mM	0.213 ml	1.063 ml	2.125 ml
  50 mM	0.043 ml	0.213 ml	0.425 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 *