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Aprepitant 阿瑞匹坦

目录号 M1650 所有产品仅供科研使用,严禁用于人或动物的治疗等任何其他用途,不为任何个人提供产品和服务  


Aprepitant是一种有效的,选择性的神经激肽-1受体(NK1R)拮抗剂,可用于恶心呕吐的相关研究。

Aprepitant结构式

别名:MK-0869, L-754030, Emend

规格 价格 库存状态
Free Sample (0.5-1 mg)  ¥ 0 中国库存现货
10mM*1mL ¥ 700 中国库存现货
5mg ¥ 550 中国库存现货
10mg ¥ 800 中国库存现货
50mg ¥ 3000 中国库存现货
100mg ¥ 4400 中国库存现货
其他规格数量报价?

质量标准及产品资料
生物活性

Aprepitant是一种有效的,选择性的神经激肽-1受体(NK1R)拮抗剂,可用于恶心呕吐的相关研究。

实验参考
体外实验*
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

*上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。

体内实验*
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.

*上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。

化学性质
分子量 534.43
分子式 C23H21F7N4O3
CAS号 170729-80-3
溶解性(25°C) DMSO 90 mg/mL
储存条件 2-8°C, protect from light
运输方式 冰袋运输,根据产品的不同,可能会有相应调整。
储备液配制

*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前,需考虑其在不同溶剂中的溶解度限制。

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
不同实验动物依据体表面积的等效剂量转换表(参考来源于公开文献
小鼠 大鼠 豚鼠 仓鼠
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。

参考文献

[1] Albany et al. J Clin Oncol. Randomized, double-blind, placebo-controlled, phase III cross-over study evaluating the oral neurokinin-1 antagonist aprepitant in combination with a 5HT3 receptor antagonist and dexamethasone in patients with germ cell tumors receiving 5-day cisplatin combination chemotherapy regimens: a hoosier oncology group study.

[2] Stiff et al. Biol Blood Marrow Transplant. Prevention of Nausea and Vomiting Associated with Stem Cell Transplantation: Results of a Prospective, Randomized Trial of Aprepitant used with Highly Emetogenic Preparative Regimens.

[3] Bergese et al. Trials. Aprepitant versus ondansetron in preoperative triple-therapy treatment of nausea and vomiting in neurosurgery patients: study protocol for a randomized controlled trial.

[4] Green et al. Br J Anaesth. Randomized, double-blind comparison of oral aprepitant alone compared with aprepitant and transdermal scopolamine for prevention of postoperative nausea and vomiting.

[5] Longo et al. Int J Clin Pract. Combination of aprepitant, palonosetron and dexamethasone as antiemetic prophylaxis in lung cancer patients receiving multiple cycles of cisplatin-based chemotherapy.

[6] Munoz M, et al. Invest New Drugs. The NK-1 receptor antagonist aprepitant as a broad spectrum antitumor drug.

[7] Tattersall FD, et al. Neuropharmacology. 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.

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