Aprepitant是一种新型的、高选择性的神经激肽-1 （NK-1）受体拮抗剂。
Cas No.:170729-80-3
Sample solution is provided at 25 µL, 10mM.
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Aprepitant is a novel and highly selective Neurokinin-1 (NK-1) receptor antagonist[1]. Aprepitant has a Kd value of 86pM for the human NK-1 receptor, and IC50 values of 0.1nM, 4nM, and 0.7nM for human, rat, and ferret NK-1 receptors, respectively[2].
In vitro, treatment with Aprepitant (5-30μM) for 24-48h exerted cytotoxic and anti-proliferative effects on Nalm-6 cells in a dose- and time-dependent manner[3]. IC50 for Aprepitant against HEK 293 cells was >90μM[2]. Aprepitant, at 10-60mM concentrations for 72h, elicits cell growth inhibition in a concentration-dependent manner in all melanoma cell lines[4].
In vivo, Intraperitoneal administration of aprepitant (10mg/kg/d) for 3 days attenuated the expression of Conditioned place preference (CPP) induced by psychostimulants, AMPH and cocaine while enhancing morphine induced CPP[5].
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 M, Rosso M. The NK-1 receptor antagonist aprepitant as a broad spectrum antitumor drug. Invest New Drugs. 2010;28(2):187-193.
[3]Bayati S, Bashash D, Ahmadian S, et al. Inhibition of tachykinin NK1 receptor using aprepitant induces apoptotic cell death and G1 arrest through Akt/p53 axis in pre-B acute lymphoblastic leukemia cells. Eur J Pharmacol. 2016;791:274-283.
[4] Muñoz M, Rosso M, Robles-Frias MJ, et al. The NK-1 receptor is expressed in human melanoma and is involved in the antitumor action of the NK-1 receptor antagonist aprepitant on melanoma cell lines. Lab Invest. 2010;90(8):1259-1269.
[5] Mannangatti P, Sundaramurthy S, Ramamoorthy S, Jayanthi LD. Differential effects of aprepitant, a clinically used neurokinin-1 receptor antagonist on the expression of conditioned psychostimulant versus opioid reward. Psychopharmacology (Berl). 2017;234(4):695-705.
Aprepitant是一种新型的、高选择性的神经激肽-1（NK-1）受体拮抗剂。Aprepitant对人NK-1受体的解离常数为86pM，对人、大鼠和雪貂NK-1受体的IC50值分别为0.1nM、0.4nM和0.7nM。
体外实验中，Aprepitant（5-30μM）处理24-48小时后，会以剂量依赖和时间依赖的方式对Nalm-6细胞产生细胞毒性和抗增殖作用[3]。Aprepitant对HEK 293细胞的IC50值大于90μM[2]。Aprepitant在10-60mM的浓度下处理72小时，对所有黑色素瘤细胞系均表现出浓度依赖性的细胞生长抑制作用[4]。
体内实验中，腹腔注射Aprepitant（10mg/kg/d），连续给药3天，可以减弱精神兴奋剂（如苯丙胺和可卡因）诱导的条件反射（CPP），同时增强吗啡诱导的条件反射[5]。
| Cell experiment [1]: | |
Cell lines | Nalm-6 |
Preparation Method | A stock solution of Aprepitant at the concentration of 10mM was prepared by dissolving the compound in 0.1% DMSO. Cells were treated with relevant amounts of the Aprepitant stock solution to attain concentration of 5, 10, 15, 20 and 30µM. In addition to the 4 negative controls (no inhibitor), cells were treated with the corresponding concentration of DMSO as an alternative negative control. |
Reaction Conditions | 5, 10, 15, 20 and 30µM; 24-36h |
Applications | Aprepitant decreased the viability and cell counts, induced rate of DNA synthesis, induced accumulation of the cells in G1 phase, and decreased the cells population in S phase in a dose- and time-dependent manner. |
| Animal experiment [2]: | |
Animal models | Male C57BL/6J mice |
Preparation Method | Aprepitant was dissolved in DMSO and diluted with saline, resulting in a final DMSO concentration of 0.002%. |
Dosage form | 10mg/kg/d; 3d; i.p. |
Applications | When compared to vehicle, Aprepitant significantly reduced the CPP expression and locomotor activation. |
References: | |
| Cas No. | 170729-80-3 | SDF | |
| 别名 | 阿瑞匹坦; MK-0869; MK-869; L-754030 | ||
| 化学名 | 5-[[(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 | ||
| Canonical SMILES | CC(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 | ||
| 分子式 | C23H21F7N4O3 | 分子量 | 534.43 |
| 溶解度 | ≥ 26.7mg/mL in DMSO | 储存条件 | 4°C, protect from light |
| General tips | 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°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8712 mL | 9.3558 mL | 18.7115 mL |
| 5 mM | 374.2 μL | 1.8712 mL | 3.7423 mL |
| 10 mM | 187.1 μL | 935.6 μL | 1.8712 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
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