Aprepitant (MK-0869) is a selective and high-affinityneurokinin 1 receptorantagonist with aK_dof 86 pM.

Kd: 86 pM (Neurokinin 1 receptor)^[1]

Aprepitant decreases the metabolic activity with an estimated IC₅₀value of 20 μM. Aprepitant induces cell-growth inhibition and G1 cell-cycle arrest. Aprepitant significantly induces apoptosis in Nalm-6 cells, and the apoptosis is mediated through caspase-3 activation. Aprepitant (20 μM) induces p53 accumulation and expression of pro-apoptotic p53 target genes^[2]. Aprepitant (1, 5, 10 μM) inhibits HIV infection in MDM from both depressed and not depressed HIV negative individuals ex vivo in a dose-dependent manner. IC₉₀value of aprepitant is equivalent to 10 μM, and the IC₅₀value is about 5 μM^[4].

Aprepitant prevents the increase of NK-1R expression induced by in vivo NHP infection withB. burgdorferi. Aprepitant treatment preventsB. burgdorferi-induced increases in CCL2 protein levels in the CSF of NHPs. Aprepitant treatment preventsB. burgdorferi-induced increases in CCL2 and CXCL13 mRNA expression in the dorsal root ganglia of NHPs, preventsB. burgdorferi-induced increases in CCL2, CXCL13, IL-17A, and IL-6 mRNA expression in the spinal cord of NHPs. Aprepitant treatment attenuatesB. burgdorferiinfection-induced reductions in astrocyte activity/numbers^[1]. Aprepitant (10 mg/kg, i.p.) significantly attenuates the CPP expression and locomotor activation produced by AMPH and cocaine in mice. In contrast, aprepitant significantly enhances the expression of CPP produced by morphine while significantly suppressing the locomotor activity of the mice conditioned with morphine. Aprepitant does not induce significant CPP or conditioned place aversion or locomotor activation or suppression^[3]. Aprepitant (125 mg/day, p.o.) results in 1 log reduction in plasma levels of viral RNA as compared to non-treated controls^[4].

534.43

Solid

C₂₃H₂₁F₇N₄O₃

170729-80-3

阿瑞匹坦；阿瑞吡坦；阿瑞比坦

Room temperature in continental US; may vary elsewhere.

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

DMSO : ≥ 100 mg/mL(187.12 mM)

*"≥" means soluble, but saturation unknown.

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

  Solubility: ≥ 2.5 mg/mL (4.68 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (4.68 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 2.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 2.5 mg/mL (4.68 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (4.68 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。