生物活性
Aprepitant是一种有效的，选择性的神经激肽-1受体拮抗剂。
化学数据
| 分子量 | 534.43 |
| 分子式 | C23H21F7N4O3 |
| CAS号 | 170729-80-3 |
| 纯度 | >99% |
| 溶解性（25°C） | DMSO 90 mg/mL |
| 储存和运输条件 | 2-8°C, protect from light
常温运输及临时存放 |
实验操作 来自于公开的文献，仅供相同实验参考（如实验材料、目的不同，请参考其他文献）
| 细胞实验 |
|---|
| 细胞系 | human CAPAN pancreas, HEp-2 larynx, gastric 23132-87 and SW-403 colon carcinoma cells |
| 方法 | Proliferation assays.
Cell proliferation was evaluated using the tetrazolium compound 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)2-(4-sulfophenyl)-2H-tetrazolium, inner salt (MTS), according to the manufacturer’s instructions (CellTiter 96 Aqueous One Solution Cell Proliferation Assay). Cell numbers were quantified using a Coulter counter. Cells were cultured in 96-well plates: each well contained 104 cells in a total volume of 100 μl. Each assay included one plate The plate included blank wells (0 cells/0.1 ml), control wells (104 cells /0.1 ml), control wells with acetonitrylo, control wells treated with aprepitant and control wells treated with the most effective SP concentration and aprepitant. The plates were inoculated with aprepitant (5–70 μM for tumor cell lines) and were incubated for the first doubling time specific for each tumor cell line. The plates were also inoculated the most mitogenic exogenous SP nM concentration with the fifty-percent inhibition concentration (IC50) of aprepitant μM concentration approximately and without aprepitant for their first doubling times respectively. For the proliferation assay, 20 μl of the MTS reagent was added to each well 90 min before reading the samples on a multiscanner microplate reader (TECAN Spectra classic, Barcelona, Spain) at 492 nm. The quantity of product, as measured by optical density, is directly proportional to the number of living cells. |
| 浓度 | 5-70 μM |
| 处理时间 | 2 days |
| 动物实验 |
|---|
| 动物模型 | acute cisplatin-induced emesis in ferrets |
| 配制 | Methocel or PEG 300 |
| 剂量 | 0.3, 1, 3mg/kg |
| 给药处理 | p.o. or i.v. |
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
| 动物 A的Km系数 |
例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。
储备液配制
以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.8712 mL | 9.3558 mL | 18.7115 mL |
| 5 mM | 0.3742 mL | 1.8712 mL | 3.7423 mL |
| 10 mM | 0.1871 mL | 0.9356 mL | 1.8712 mL |
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