GLPBio

Aprepitant

Catalog No.: GC15200Purity:>99.50%Synonyms: Emend, L754,030, MK-869, ONO7436
COASDSData Sheet
Aprepitant is a novel and highly selective Neurokinin-1 (NK-1) receptor antagonist.

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Aprepitant
Cas No.: 170729-80-3
10mM (in 1mL DMSO)In Stock
$62.00
1
1mgIn Stock
$24.00
1
5mgIn Stock
$53.00
1
10mgIn Stock
$74.00
1
25mgIn Stock
$133.00
1
50mgIn Stock
$192.00
1
100mgIn Stock
$269.00
1
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Description

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.

Protocol

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:
[1]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.
[2] 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.

Product Documents

Purity:>99.50%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
170729-80-3
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
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
Molecular Formula
C23H21F7N4O3
Molecular Weight
534.43
Solubility
≥ 26.7mg/mL in DMSO
Storage
4°C, protect from light
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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