简介：Aprepitant (MK-0869) is a selective and high-affinityneurokinin1 receptorantagonist with aKdof 86pM.
物理性状及指标：
外观：……………………粉末
溶解性：…………………DMSO：100mg/mL(187.12 mM)
含量：……………………>98%
生物活性（仅来自于公开文献，不保证其有效性）
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描述 |
Aprepitant (MK-0869) is a selective and high-affinityneurokinin 1 receptorantagonist with aKdof 86 pM. |
|
靶点 |
Kd: 86 pM (Neurokinin 1 receptor) |
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体外 |
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. 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 |
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体内 |
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. 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. Aprepitant (125 mg/day, p.o.) results in 1 log reduction in plasma levels of viral RNA as compared to non-treated controls |
储液配置及储存：按表中溶解性配置；如溶解困难或者有析出，可以通过快速搅拌，超声或温和加热（在45-60°C下水浴）。液体稳定性报道的很少，建议现配现用，如需储存，建议：-20℃1-3月；-80℃ 3-6月。
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浓度/体积DMSO/质量 |
1 mg |
5 mg |
10 mg |
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1 mM |
1.8712 mL |
9.3558 mL |
18.7115 mL |
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5 mM |
0.3742 mL |
1.8712 mL |
3.7423 mL |
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10 mM |
0.1871 mL |
0.9356 mL |
1.8712 mL |
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