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Aprepitant Sale

(Synonyms: 阿瑞匹坦; MK-0869; MK-869; L-754030) 目录号 : GC15200

An antiemetic and NK1 antagonist

Aprepitant Chemical Structure

Cas No.:170729-80-3

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥654.00
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5mg
¥586.00
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25mg
¥1,615.00
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100mg
¥3,638.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Cell experiment [1]:

Cell lines

Nalm-6 cells

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.

Reacting condition

20 μM

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]:

Animal models

Male C57BL/6J mice

Dosage form

Intraperitoneal injection, 10 mg/kg

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.

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.

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.

产品描述

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.

Chemical Properties

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。
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。

溶解性数据

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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
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