Aprepitant
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Aprepitant（也称MK-0869）是一种新的具有高度选择性的Neurokinin-1（NK-1）受体抑制剂，可在NK-1受体上抑制P物质（SP）的活性（P物质是一种十一肽，属于速激肽家族），对人NK-1受体的解离常数Kd为86 pM，对人类、大鼠和雪貂NK-1受体的半数最大抑制浓度IC50值分别为0.1 nM、4 nM和0.7 nM[1,2]。
由于SP被证明可在多种过表达NK-1受体的人类癌细胞系中抑制细胞增殖，aprepitant以浓度不依赖的方式在多种肿瘤细胞系中诱导生长抑制，包括胶质瘤（GAMG）、神经母细胞瘤（SKN-BE2、IMR-32和KELLY）、视网膜母细胞瘤（Y-79和WERI-Rb-1）、胰腺癌（PA-TU-8902和CAPAN-1）和结肠癌（SW-403），IC50值分别为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和30.5 μΜ[2]。
参考文献：
[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] Muoz 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.
- 1. Kwatra SG, Boozalis E, et al. "Proteomic and Phosphoproteomic Analysis Reveals that Neurokinin-1 Receptor (NK1R) Blockade with Aprepitant in Human Keratinocytes Activates a Distinct Subdomain of EGFR Signaling: Implications for the Anti-Pruritic Activity of NK1R Antagonists." Medicines (Basel). 2019 Dec 9;6(4). pii: E114. PMID:31835310
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 534.43 |
| Cas No. | 170729-80-3 |
| Formula | C23H21F7N4O3 |
| Solubility | ≥26.72 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
| Chemical Name | 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 |
| SDF | Download SDF |
| 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 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验 [1]: | |
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细胞系 |
Nalm-6细胞 |
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溶解方法 |
该化合物在DMSO中的溶解度大于26.7 mg/mL。若获取更高浓度的溶液，可在37℃下孵育10分钟，随后在超声波浴中摇匀。-20℃以下可储存数月。 |
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反应条件 |
20 μM |
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应用 |
Aprepitant降低代谢活性，IC50值大约为20 μM。Aprepitant抑制细胞生长和G1细胞周期停滞。Aprepitant显著诱导Nalm-6细胞凋亡。Aprepitant（20 μM）诱导p53的积累和促凋亡p53靶基因的表达。 |
| 动物实验[2]: | |
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动物模型 |
雄性C57BL/6J小鼠 |
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给药剂量 |
腹腔注射10 mg/kg |
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应用 |
在小鼠中，腹腔注射Aprepitant（10 mg/kg）显著减弱AMPH诱导的CPP表达以及AMPH和可卡因诱导的运动活化。Aprepitant显著增强吗啡引起的CPP表达，而显著抑制吗啡调节的小鼠的运动活性。 |
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注意事项 |
由于实验环境的不同，实际溶解度可能与理论值略有不同，请测试室内所有化合物的溶解度。 |
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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. |
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质量控制和MSDS
- 批次:
化学结构
