产品说明书
Aprepitant
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同义名 : | 阿瑞吡坦 ;MK-0869;MK-869;US brand name: Emend;ONO-7436;Emend;L-754030 |
| CAS号 : | 170729-80-3 | |
| 货号 : | A103179 | |
| 分子式 : | C23H21F7N4O3 | |
| 纯度 : | 98% | |
| 分子量 : | 534.427 | |
| MDL号 : | MFCD08277635 | |
| 存储条件： |
粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 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 |
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| 动物实验配方： |
| 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]. | ||
| 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 | ||
| 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) | - | - | |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.87mL 0.37mL 0.19mL |
9.36mL 1.87mL 0.94mL |
18.71mL 3.74mL 1.87mL |
| 参考文献 |
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