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首页 / 抑制剂/激动剂 / 神经信号通路 /
NK Receptor
Substance P
/ Aprepitant

阿瑞匹坦 /Aprepitant {[allProObj[0].p_purity_real_show]}

货号：A103179 同义名： 阿瑞吡坦 / MK-0869;MK-869

Aprepitant is a selective and high-affinity neurokinin-1 receptor antagonist with IC50 of 0.1 nM.

Aprepitant 化学结构 CAS号：170729-80-3
Aprepitant 化学结构
CAS号：170729-80-3
Aprepitant 3D分子结构
CAS号：170729-80-3
Aprepitant 化学结构 CAS号：170729-80-3
Aprepitant 3D分子结构 CAS号：170729-80-3
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Aprepitant 纯度/质量文件 产品仅供科研

货号：A103179 标准纯度： {[allProObj[0].p_purity_real_show]}
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Aprepitant 生物活性

描述 Neurokinin family is a group of neurotransmitters that functions through the G-protein-coupled neurokinin receptors. Aprepitant is an antagonist for Neurokinin-1 (NK1) receptor with a Ki value of 3 nM and a IC50 value of 0.09 nM for human NK1[5]. Aprepitant is 3000-fold selective for human NK1 over human NK3, and > 50000-fold selective versus human NK2. Intravenous administration of 1 and 3 mg/kg aprepitant dose-dependently and significantly suppressed emesis response to cisplatin in ferrets during 4-hour observation, whereas oral administration of 0.3 – 3 mg/kg aprepitant significantly restrained cisplatin-induced retching and vomiting. The emetic activity was inhibited by intravenous injection of aprepitant (0.3 – 3 mg/kg) with the flattening of cumulative numbers of retches occurring in the 4-hour observation period. The anti-emetic activity of aprepitant (0.1 mg/kg, i.v.) was increased with the combination of ondansetron (0.1 mg/kg, i.v.) and dexamethasone (20 mg/kg, i.v.). In the 6 animals treated with aprepitant and dexamethasone, one showed complete inhibition of retching and vomiting for the 4-hour observation period. One oral dose of aprepitant (4, 8, and 16 mg/kg) 2 hours before cisplatin (5 mg/kg, i.p.) stimulation, the retching and vomiting response were dose-dependently suppressed during the 72-hour observation[6].
作用机制 Aprepitant acts as an antagonist for NK1 by inhibiting the binding of substance P to the NK1 receptor[7].

Aprepitant 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
CHO cells Function assay Displacement of [125I]SP from human NK1 receptor expressed in CHO cells, IC50=9e-05 μM 17723300
HEK293 cell Function assay Displacement of [125I]-substance P from gerbil NK1 receptor expressed in HEK293 cell membranes incubated for 30 mins by liquid scintillation counting method, IC50=9e-05 μM 26048800
HEK293 cell Function assay Noncompetitive inhibition of wild type human NK1 receptor expressed in HEK293 cells assessed as decrease in SP1-induced [3H]IP accumulation after 20 mins 22574973

Aprepitant 动物研究

Dose Rat: 1 mg/ml/rat[3] (i.v.)
Administration i.v.
Pharmacokinetics
Animal Rats[4]
Dose 5 mg/kg
Administration i.v.
T1/2 2.4 h
CL 13.4 ml/min/kg
Vdss 2.5 L/kg
AUC0→∞ 6377 ng·h/ml

Aprepitant 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00428519 HIV Infections Phase 1 Completed - United States, Pennsylvania ... 展开 >> Clinical Trials Unit. University of Pennsylvania Philadelphia, Pennsylvania, United States, 19104 收起 <<
NCT01757210 - Completed - United States, West Virginia ... 展开 >> WVU Healthcare Morgantown, West Virginia, United States, 26506 收起 <<
NCT01405924 - Terminated(Low enrollment) - -

Aprepitant 参考文献

[1]Navari RM. Aprepitant: a neurokinin-1 receptor antagonist for the treatment of chemotherapy-induced nausea and vomiting. Expert Rev Anticancer Ther. 2004 Oct;4(5):715-24.

[2]Tattersall FD, Rycroft W, et al. 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.

[3]Cinvanti

[4]L 754030

[5]Finke PE, Meurer LC, Levorse DA, Mills SG, Maccoss M, Sadowski S, Cascieri MA, Tsao KL, Chicchi GG, Metzger JM, Macintyre DE. Cyclopentane-based human NK1 antagonists. Part 1: discovery and initial SAR. Bioorg Med Chem Lett. 2006 Sep 1;16(17):4497-503.

[6]Tattersall FD, 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.

[7]Bissantz C, Bohnert C, Hoffmann T, Marcuz A, Schnider P, Malherbe P. Identification of a crucial amino acid in the helix position 6.51 of human tachykinin neurokinin 1 and 3 receptors contributing to the insurmountable mode of antagonism by dual NK₁/NK₃ antagonists. J Med Chem. 2012 Jun 14;55(11):5061-76.

Aprepitant 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.87mL

0.37mL

0.19mL

9.36mL

1.87mL

0.94mL

18.71mL

3.74mL

1.87mL

Aprepitant 技术信息

CAS号170729-80-3
分子式C23H21F7N4O3
分子量 534.427
别名 阿瑞吡坦 ;MK-0869;MK-869;US brand name: Emend;ONO-7436;Emend;L-754030
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C
溶解度

DMSO: 105 mg/mL(196.47 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: Aprepitant | MK-0869;MK-869;ONO-7436;Emend;L-754030 | 阿瑞吡坦 | NK Receptor | Substance P | AmBeed-信号通路专用抑制剂 | Aprepitant 纯度/质量文件 | Aprepitant 生物活性 | Aprepitant 细胞研究 | Aprepitant 动物研究 | Aprepitant 临床数据 | Aprepitant 参考文献 | Aprepitant 实验方案 | Aprepitant 技术信息

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