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• 产品描述： Netupitant is a specific neurokinin 1 (NK1) receptor antagonist (Ki: 0.95 nM).

• 靶点： Neurokinin receptor

• 体内研究： In mice the intrathecal injection of SP elicited the typical scratching, biting and licking response is dose-dependently inhibited by Netupitant (1-10 mg/kg, i.p.). In gerbils, foot tapping behavior evoked by the intracerebroventricular injection of an NK1 agonist is dose-dependently counteracted by Netupitant gave intraperitoneally (ID50 1.5 mg/kg) or orally (ID50 0.5 mg/kg). In time course experiments in gerbils, Netupitant displayed long-lasting effects.

• 细胞实验： Cell lines: NG108-15 cells. Concentrations: 1,3,10,30 nM. Method:cells are preincubated for 1 h at 37℃ with either growth media alone(control) or media containing antagonists.Antagonist concentrations are at least 30-fold the Kd value to ensure receptor saturation.After preincubation,antagonists are removed and cells are rinsed with growth media alone for an additional hour to allow for dissociation of antagonists still bound to the receptor.Cell media are then replaced with isosmotic HEPES buffer (pH 7.4,20 mM) containing NaCl (130 mM),KCl (2 mM),MgCl2 (1 mM) CaCl2 (2 mM),Fluo-4 acetoxymethyl (AM) ester (2 mM),pluronic acid (0.04%) and SP at various concentrations in the 3 nM to 1 mM range.The final incubation lasted for 1 h at 37 ℃.Pluronic acid is added as a nonionic surfactant to sequester the AM ester molecules into micelles for cellular uptake.

• 动物实验： Animal Models: Male Swiss mice. Formulation: Saline containing 5% DMSO and 5% Tween 80. Dosages: 1 and 10 mg/kg. Administration: i.p.

• 参考文献：
  1. Rizzi A, et al. Peptides. 2012, 37(1):86-97. 2. Stathis M, et al. Eur J Pharmacol. 2012, 689(1-3):25-30.

• 溶解性： Soluble  in  DMSO

• 保存条件： 2-8℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.728 ml	8.642 ml	17.283 ml
  5 mM	0.346 ml	1.728 ml	3.457 ml
  10 mM	0.173 ml	0.864 ml	1.728 ml
  50 mM	0.035 ml	0.173 ml	0.346 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 分子量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *