Aprepitant
(Synonyms: 阿瑞匹坦; MK-0869; MK-869; L-754030) 目录号 : GC15200
An antiemetic and NK1 antagonist
Cas No.:170729-80-3
Sample solution is provided at 25 µL, 10mM.
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Aprepitant (also known as MK-0869) is a novel and highly selective Neurokinin-1 (NK-1) receptor antagonist that inhibits the activity of substance P (SP), an undecapeptide belonging to the tachykinin family of peptides, on the NK-1 receptor with the dissociation constant Kd of 86 pM for human NK-1 receptor and the half maximal inhibition concentration IC50 of 0.1 nM, 4 nM and 0.7 nM for human, rat and ferret NK-1 receptors respectively [1,2].
Since SP has been demonstrated to induce cell proliferation in several human cancer cell lines with overexpressed NK-1 receptors, aprepitant has also been found to concentration-dependently induce growth inhibition in a variety of tumor cell lines, including glioma (GAMG), neuroblastoma (SKN-BE2, IMR-32 and KELLY), retinoblastoma (Y-79 and WERI-Rb-1), pancreas carcinoma (PA-TU-8902 and CAPAN-1), larynx carcinoma (HEp-2), gastric carcinoma (23132-87) and colon carcinoma (SW-403), with IC50 of 33.1 μΜ, 24.6 μΜ, 19.6 μΜ, 27.7 μΜ, 30.4 μΜ, 23 μΜ, 31.2 μΜ, 27.4 μΜ, 22.7 μΜ, 24.2 μΜ and 30.5 μΜ respectively [2].
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 M1, Rosso M. The NK-1 receptor antagonist aprepitant as a broad spectrum antitumor drug. Invest New Drugs. 2010 Apr;28(2):187-93. doi: 10.1007/s10637-009-9218-8. Epub 2009 Jan 17.
| Cell experiment [1]: | |
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Cell lines |
Nalm-6 cells |
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Preparation method |
The solubility of this compound in DMSO is >26.7mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
20 μM |
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Applications |
Aprepitant decreased the metabolic activity with an estimated IC50 value of 20 μM. Aprepitant induced cell-growth inhibition and G1 cell-cycle arrest. Aprepitant significantly induced apoptosis in Nalm-6 cells. Aprepitant (20 μM) induced p53 accumulation and expression of pro-apoptotic p53 target genes. |
| Animal experiment [2]: | |
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Animal models |
Male C57BL/6J mice |
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Dosage form |
Intraperitoneal injection, 10 mg/kg |
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Application |
Aprepitant (10 mg/kg, i.p.) significantly attenuated AMPH-induced CPP expression and locomotor activation produced by AMPH and cocaine in mice. Aprepitant significantly enhanced the expression of CPP produced by morphine while significantly suppressing the locomotor activity of the mice conditioned with morphine. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Bayati S, Bashash D, Ahmadian S, et al. Inhibition of tachykinin NK 1 receptor using aprepitant induces apoptotic cell death and G1 arrest through Akt/p53 axis in pre-B acute lymphoblastic leukemia cells[J]. European journal of pharmacology, 2016, 791: 274-283. [2]. Mannangatti P, Sundaramurthy S, Ramamoorthy S, et al. Differential effects of aprepitant, a clinically used neurokinin-1 receptor antagonist on the expression of conditioned psychostimulant versus opioid reward[J]. Psychopharmacology, 2017, 234(4): 695-705. | |
| 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 | 0.3742 mL | 1.8712 mL | 3.7423 mL |
| 10 mM | 0.1871 mL | 0.9356 mL | 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
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet