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Aprepitant

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Catalog No.
A1684
P物质(SP)抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 770.00
现货
5mg
¥ 690.00
现货
25mg
¥ 1,900.00
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100mg
¥ 4,280.00
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Background

Aprepitant (also known as MK-0869) is a novel and highly selective Neurokinin-1 (NK-1) receptor antagonist that inhibits the activity of substance P (SP), an undecapeptide belonging to the tachykinin family of peptides, on the NK-1 receptor with the dissociation constant Kd of 86 pM for human NK-1 receptor and the half maximal inhibition concentration IC50 of 0.1 nM, 4 nM and 0.7 nM for human, rat and ferret NK-1 receptors respectively [1,2].

Since SP has been demonstrated to induce cell proliferation in several human cancer cell lines with overexpressed NK-1 receptors, aprepitant has also been found to concentration-dependently induce growth inhibition in a variety of tumor cell lines, including glioma (GAMG), neuroblastoma (SKN-BE2, IMR-32 and KELLY), retinoblastoma (Y-79 and WERI-Rb-1), pancreas carcinoma (PA-TU-8902 and CAPAN-1), larynx carcinoma (HEp-2), gastric carcinoma (23132-87) and colon carcinoma (SW-403), with IC50 of 33.1 μΜ, 24.6 μΜ, 19.6 μΜ, 27.7 μΜ, 30.4 μΜ, 23 μΜ, 31.2 μΜ, 27.4 μΜ, 22.7 μΜ, 24.2 μΜ and 30.5 μΜ respectively [2].

References:
[1] Tattersall FD1, Rycroft W, Cumberbatch M, Mason G, Tye S, Williamson DJ, Hale JJ, Mills SG, Finke PE, MacCoss M, Sadowski S, Ber E, Cascieri M, Hill RG, MacIntyre DE, Hargreaves RJ. The novel NK1 receptor antagonist MK-0869 (L-754,030) and its water soluble phosphoryl prodrug, L-758,298, inhibit acute and delayed cisplatin-induced emesis in ferrets. Neuropharmacology. 2000 Feb 14;39(4):652-63.
[2] Muñoz M1, Rosso M. The NK-1 receptor antagonist aprepitant as a broad spectrum antitumor drug. Invest New Drugs. 2010 Apr;28(2):187-93. doi: 10.1007/s10637-009-9218-8. Epub 2009 Jan 17.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt534.43
Cas No.170729-80-3
FormulaC23H21F7N4O3
Solubility≥26.7mg/mL in DMSO
Chemical Name5-[[(2R,3S)-2-[1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholin-4-yl]methyl]-1,2-dihydro-1,2,4-triazol-3-one
SDFDownload SDF
Canonical SMILESCC(C1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)OC2C(N(CCO2)CC3=NC(=O)NN3)C4=CC=C(C=C4)F
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

Nalm-6细胞

溶解方法

该化合物在DMSO中的溶解度大于26.7 mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

反应条件

20 μM

应用

Aprepitant降低代谢活性,IC50值大约为20 μM。Aprepitant抑制细胞生长和G1细胞周期停滞。Aprepitant显著诱导Nalm-6细胞凋亡。Aprepitant(20 μM)诱导p53的积累和促凋亡p53靶基因的表达。

动物实验[2]:

动物模型

雄性C57BL/6J小鼠

给药剂量

腹腔注射10 mg/kg

应用

在小鼠中,腹腔注射Aprepitant(10 mg/kg)显著减弱AMPH诱导的CPP表达以及AMPH和可卡因诱导的运动活化。Aprepitant显著增强吗啡引起的CPP表达,而显著抑制吗啡调节的小鼠的运动活性。

注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

References:

[1]. Bayati S, Bashash D, Ahmadian S, et al. Inhibition of tachykinin NK 1 receptor using aprepitant induces apoptotic cell death and G1 arrest through Akt/p53 axis in pre-B acute lymphoblastic leukemia cells[J]. European journal of pharmacology, 2016, 791: 274-283.

[2]. Mannangatti P, Sundaramurthy S, Ramamoorthy S, et al. Differential effects of aprepitant, a clinically used neurokinin-1 receptor antagonist on the expression of conditioned psychostimulant versus opioid reward[J]. Psychopharmacology, 2017, 234(4): 695-705.

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