Aprepitant (Synonyms: Emend, L754,030, MK-869, ONO7436) |
Catalog No.GC15200
One-Click Copy Product Info
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Aprepitant is a novel and highly selective Neurokinin-1 (NK-1) receptor antagonist.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 170729-80-3
Sample solution is provided at 25 µL, 10mM.
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Aprepitant is a novel and highly selective Neurokinin-1 (NK-1) receptor antagonist[1]. Aprepitant has a Kd value of 86pM for the human NK-1 receptor, and IC50 values of 0.1nM, 4nM, and 0.7nM for human, rat, and ferret NK-1 receptors, respectively[2].
In vitro, treatment with Aprepitant (5-30μM) for 24-48h exerted cytotoxic and anti-proliferative effects on Nalm-6 cells in a dose- and time-dependent manner[3]. IC50 for Aprepitant against HEK 293 cells was >90μM[2]. Aprepitant, at 10-60mM concentrations for 72h, elicits cell growth inhibition in a concentration-dependent manner in all melanoma cell lines[4].
In vivo, Intraperitoneal administration of aprepitant (10mg/kg/d) for 3 days attenuated the expression of Conditioned place preference (CPP) induced by psychostimulants, AMPH and cocaine while enhancing morphine induced CPP[5].
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 M, Rosso M. The NK-1 receptor antagonist aprepitant as a broad spectrum antitumor drug. Invest New Drugs. 2010;28(2):187-193.
[3]Bayati S, Bashash D, Ahmadian S, et al. Inhibition of tachykinin NK1 receptor using aprepitant induces apoptotic cell death and G1 arrest through Akt/p53 axis in pre-B acute lymphoblastic leukemia cells. Eur J Pharmacol. 2016;791:274-283.
[4] Muñoz M, Rosso M, Robles-Frias MJ, et al. The NK-1 receptor is expressed in human melanoma and is involved in the antitumor action of the NK-1 receptor antagonist aprepitant on melanoma cell lines. Lab Invest. 2010;90(8):1259-1269.
[5] Mannangatti P, Sundaramurthy S, Ramamoorthy S, Jayanthi LD. Differential effects of aprepitant, a clinically used neurokinin-1 receptor antagonist on the expression of conditioned psychostimulant versus opioid reward. Psychopharmacology (Berl). 2017;234(4):695-705.
| Cell experiment [1]: | |
Cell lines | Nalm-6 |
Preparation Method | A stock solution of Aprepitant at the concentration of 10mM was prepared by dissolving the compound in 0.1% DMSO. Cells were treated with relevant amounts of the Aprepitant stock solution to attain concentration of 5, 10, 15, 20 and 30µM. In addition to the 4 negative controls (no inhibitor), cells were treated with the corresponding concentration of DMSO as an alternative negative control. |
Reaction Conditions | 5, 10, 15, 20 and 30µM; 24-36h |
Applications | Aprepitant decreased the viability and cell counts, induced rate of DNA synthesis, induced accumulation of the cells in G1 phase, and decreased the cells population in S phase in a dose- and time-dependent manner. |
| Animal experiment [2]: | |
Animal models | Male C57BL/6J mice |
Preparation Method | Aprepitant was dissolved in DMSO and diluted with saline, resulting in a final DMSO concentration of 0.002%. |
Dosage form | 10mg/kg/d; 3d; i.p. |
Applications | When compared to vehicle, Aprepitant significantly reduced the CPP expression and locomotor activation. |
References: | |
| Cas No. | 170729-80-3 | SDF | |
| Synonyms | Emend, L754,030, MK-869, ONO7436 | ||
| 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 | ||
| 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 | ||
| Formula | C23H21F7N4O3 | M.Wt | 534.43 |
| Solubility | ≥ 26.7mg/mL in DMSO | Storage | 4°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8712 mL | 9.3558 mL | 18.7115 mL |
| 5 mM | 374.2 μL | 1.8712 mL | 3.7423 mL |
| 10 mM | 187.1 μL | 935.6 μL | 1.8712 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)