Cat. No.: HY-10052

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Aprepitant

(Synonyms: MK-0869; MK-869; L-754030)

13 Cited Publications

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Based on 13 publication(s) in Google Scholar

Aprepitant (MK-0869) is a selective and high-affinity neurokinin 1 receptor antagonist with a K_d of 86 pM.

For research use only. We do not sell to patients.

Purity: 99.82%
CAS No.: 170729-80-3
Formula: C₂₃H₂₁F₇N₄O₃
Molecular Weight:534.43

Storage:

4°C, protect from light

* In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

Aprepitant Chemical Structure

CAS No.: 170729-80-3

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (13)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

Aprepitant (MK-0869) is a selective and high-affinity neurokinin 1 receptor antagonist with a K_d of 86 pM.

IC₅₀ & Target

Kd: 86 pM (Neurokinin 1 receptor)^[1]

All Neurokinin Receptor Isoforms :

All HIV Isoforms :

All Antibiotic Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	18.3 μM Compound: Aprepitant	Anti-cancer activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Anti-cancer activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 34236855]
A549	IC₅₀	18.3 μM Compound: Aprepitant	Anti-cancer activity against human A549 cells incubated for 96 hrs by Resazurin assay Anti-cancer activity against human A549 cells incubated for 96 hrs by Resazurin assay	[PMID: 34236855]
CHO	IC₅₀	0.09 nM Compound: 1, Aprepitant	Displacement of [125I]SP from human cloned NK1 receptor expressed in CHO cells Displacement of [125I]SP from human cloned NK1 receptor expressed in CHO cells	[PMID: 16824752]
CHO	IC₅₀	0.09 nM Compound: 1, Aprepitant	Displacement of [125I]SP from human cloned NK1 receptor expressed in CHO cells Displacement of [125I]SP from human cloned NK1 receptor expressed in CHO cells	[PMID: 16831551]
CHO	IC₅₀	0.09 nM Compound: 1, aprepitant	Displacement of [125I]SP from human NK1 receptor expressed in CHO cells Displacement of [125I]SP from human NK1 receptor expressed in CHO cells	[PMID: 17723300]
CHO	IC₅₀	0.09 nM Compound: 17	Displacement of [125I]-labeled SP from the human Tachykinin receptor 1 expressed in CHO cells Displacement of [125I]-labeled SP from the human Tachykinin receptor 1 expressed in CHO cells	[PMID: 9804700]
HEK293	IC₅₀	0.09 nM Compound: 1	Displacement of [125I]-substance P from gerbil NK1 receptor expressed in HEK293 cell membranes incubated for 30 mins by liquid scintillation counting method Displacement of [125I]-substance P from gerbil NK1 receptor expressed in HEK293 cell membranes incubated for 30 mins by liquid scintillation counting method	[PMID: 26048800]
Kelly	IC₅₀	15.1 μM Compound: Aprepitant	Cytotoxicity against human Kelly cells assessed as inhibition of cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human Kelly cells assessed as inhibition of cell viability incubated for 72 hrs by MTT assay	[PMID: 38086194]
MRC5	IC₅₀	28.9 μM Compound: Aprepitant	Anti-cancer activity against human MRC5 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Anti-cancer activity against human MRC5 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 34236855]
TERT-RPE1	IC₅₀	176.3 μM Compound: Aprepitant	Cytotoxicity against human RPE-1 cells assessed as inhibition of cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human RPE-1 cells assessed as inhibition of cell viability incubated for 72 hrs by MTT assay	[PMID: 38086194]

In Vitro

Aprepitant decreases the metabolic activity with an estimated IC₅₀ value of 20 μM. Aprepitant induces cell-growth inhibition and G1 cell-cycle arrest. Aprepitant significantly induces apoptosis in Nalm-6 cells, and the apoptosis is mediated through caspase-3 activation. Aprepitant (20 μM) induces p53 accumulation and expression of pro-apoptotic p53 target genes^[2]. Aprepitant (1, 5, 10 μM) inhibits HIV infection in MDM from both depressed and not depressed HIV negative individuals ex vivo in a dose-dependent manner. IC₉₀ value of aprepitant is equivalent to 10 μM, and the IC₅₀ value is about 5 μM^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Aprepitant prevents the increase of NK-1R expression induced by in vivo NHP infection with B. burgdorferi. Aprepitant treatment prevents B. burgdorferi-induced increases in CCL2 protein levels in the CSF of NHPs. Aprepitant treatment prevents B. burgdorferi-induced increases in CCL2 and CXCL13 mRNA expression in the dorsal root ganglia of NHPs, prevents B. burgdorferi-induced increases in CCL2, CXCL13, IL-17A, and IL-6 mRNA expression in the spinal cord of NHPs. Aprepitant treatment attenuates B. burgdorferi infection-induced reductions in astrocyte activity/numbers^[1]. Aprepitant (10 mg/kg, i.p.) significantly attenuates the CPP expression and locomotor activation produced by AMPH and cocaine in mice. Aprepitant does not induce significant CPP or conditioned place aversion or locomotor activation or suppression^[3]. Aprepitant (125 mg/day, p.o.) results in 1 log reduction in plasma levels of viral RNA as compared to non-treated controls^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 170729-80-3
Appearance Solid
Molecular Weight 534.43
Formula C₂₃H₂₁F₇N₄O₃
Color White to off-white
SMILES

O=C1NC(CN2[C@H]([C@@H](O[C@@H](C3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)C)OCC2)C4=CC=C(F)C=C4)=NN1
Synonyms

MK-0869; MK-869; L-754030
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

* In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

Publications (13)

All WBApoptosis AnalysisCell Proliferation/Viability AssayIP

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Journal Impact Factor

Cell Death Dis

Neurokinin-1 receptor drives PKCɑ-AURKA/N-Myc signaling to facilitate the neuroendocrine progression of prostate cancer. [Abstract]

2023 Jun 29;14(6):384. PMID: 37385990

Aprepitant purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Jun 29;14(6):384. [Abstract]

AURKA phosphorylation level was reduced by Aprepitant and GF109203X treatment in 22Rv1-NE and LNCaP-NE cells. The cells were pre-treated with Aprepitant (2 μM) or GF109203X for 30 min and stimulated by 1 μM hHK-1 for 30 min before subjecting to western blot analysis.
Cell Death Dis

Neurokinin-1 receptor promotes non-small cell lung cancer progression through transactivation of EGFR. [Abstract]

2022 Jan 10;13(1):41. PMID: 35013118

Aprepitant purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 Jan 10;13(1):41. [Abstract]

Aprepitant (20-40 μM; 24 h). Aprepitant treatment induced NSCLC cell apoptosis measured by flow cytometry analysis of PI/Annexin V co-staining.

Aprepitant purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 Jan 10;13(1):41. [Abstract]

Aprepitant (0-40 μM; 72 h). Aprepitant inhibited the ability of cell colony formation stimulated by hHK-1.

Aprepitant purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 Jan 10;13(1):41. [Abstract]

Aprepitant (0-20 μM; 24 h). Co-immunoprecipitation assay by the antibody of NK1R or EGFR to show NK1R-EGFR interaction in A549 cell lines. Cells were treated with hHK-1 or Aprepitant for 24 h to detect the effect on NK1R-EGFR interaction.

Aprepitant purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 Jan 10;13(1):41. [Abstract]

Aprepitant (0-40 μM; 72 h). Cell viability of A549 treated with Apre and Osim/Gefi at indicated concentrations.
Liver Int

Neurokinin-1 receptor antagonist aprepitant regulates autophagy and apoptosis via ROS/JNK in intrahepatic cholangiocarcinoma. [Abstract]

2024 Jul;44(7):1651-1667. PMID: 38554043
Sci Rep

Metapanax delavayi extract as a neurocutaneous modulator via CRHR1/POMC/MC1R signaling. [Abstract]

2026 Feb 9;16(1):7851. PMID: 41663512
Sci Rep

Single-cell and bulk transcriptomics uncovers PRKD2-driven tumor stemness and progression in multiple myeloma. [Abstract]

2025 Oct 21;15(1):36723. PMID: 41120632
Korean J Pain

Anti-nociceptive effects of dual neuropeptide antagonist therapy in mouse model of neuropathic and inflammatory pain. [Abstract]

2022 Apr 1;35(2):173-182. PMID: 35354680
Front Pain Res

Spontaneous, Voluntary, and Affective Behaviours in Rat Models of Pathological Pain. [Abstract]

2021 Jul 1:2:672711. PMID: 35295455
Uppsala University

2024.
Research Square Print

2023 Mar 2.
Research Square Print

2023 Feb 2.
Research Square Preprint

2021 Sep.
Research Square Preprint

2021 Jul.
Oxid Med Cell Longev

Reactive Oxygen Species Mediate Low Back Pain by Upregulating Substance P in Intervertebral Disc Degeneration. [Abstract]

2021 May 14:2021:6681815. PMID: 34093962

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (93.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: Corn Oil

Solubility: 10 mg/mL (18.71 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocol

Cell Assay^[2]

The inhibitory effect of aprepitant on metabolic activity of Nalm-6 cells is assessed by uptake of thiazolyl blue tetrazolium bromide (MTT) by viable cells. Cells are plated onto 96-well plates at a density of 5000 cells/well. After treatment with aprepitant at 5, 10, 15, 20 and 30 µM for 24, 36 and 48 h, the cells are further incubated with 100 μL of MTT (0.5 mg/mL) at 37°C for 3 h. Untreated cells are defined as the control group. Following solubilization of precipitated formazan with 100 μL of DMSO, the optical densitometry is measured with an ELISA reader at a wavelength of 578 nm.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]

Fifteen rhesus macaques are anesthetized and inoculated intrathecally with 1×10⁸ live spirochetes into the cisterna magna, whereas five rhesus macaques are left uninfected and receive 1 mL of RPMI 1640 medium after removing an equivalent volume of CSF. The establishment of in vivo B. burgdorferi infection is confirmed by positive culture from at least necropsy tissue sample. The first set of animals are studied for 2 weeks and included two control animals (one of which is treated with aprepitant), two infected and untreated animals, and two infected animals that are treated with aprepitant. The second set of animals are studied for 4 weeks and included three control animals (one of which is treated with aprepitant), five infected and untreated animals, and four infected animals treated with aprepitant. Animals receive an average dose of aprepitant of 28 ± 6 mg/kg per day p.o. daily, and drug treatments are started 2 days before inoculation. These doses are consistent with standard veterinary regimens for the chosen drugs in NHP, and the 4-week duration of the study precludes the development of neural pathology that occurs at 8 weeks following B. burgdorferi infection.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Martinez AN, et al. Aprepitant limits in vivo neuroinflammatory responses in a rhesus model of Lyme neuroborreliosis. J Neuroinflammation. 2017 Feb 15;14(1):37. [Content Brief]

[2]. Bayati 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 Nov 15;791:274-283. [Content Brief]

[3]. Mannangatti P, et al. Differential effects of aprepitant, a clinically used neurokinin-1 receptor antagonist on the expression of conditioned psychostimulant versus opioid reward. Psychopharmacology (Berl). 2017 Feb;234(4):695-705. [Content Brief]

[4]. Barrett JS, et al. Pharmacologic rationale for the NK1R antagonist, aprepitant as adjunctive therapy in HIV. J Transl Med. 2016 May 26;14(1):148. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8712 mL	9.3558 mL	18.7115 mL	46.7788 mL
	5 mM	0.3742 mL	1.8712 mL	3.7423 mL	9.3558 mL
	10 mM	0.1871 mL	0.9356 mL	1.8712 mL	4.6779 mL
	15 mM	0.1247 mL	0.6237 mL	1.2474 mL	3.1186 mL
	20 mM	0.0936 mL	0.4678 mL	0.9356 mL	2.3389 mL
	25 mM	0.0748 mL	0.3742 mL	0.7485 mL	1.8712 mL
	30 mM	0.0624 mL	0.3119 mL	0.6237 mL	1.5593 mL
	40 mM	0.0468 mL	0.2339 mL	0.4678 mL	1.1695 mL
	50 mM	0.0374 mL	0.1871 mL	0.3742 mL	0.9356 mL
	60 mM	0.0312 mL	0.1559 mL	0.3119 mL	0.7796 mL
	80 mM	0.0234 mL	0.1169 mL	0.2339 mL	0.5847 mL

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Aprepitant

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Publications Citing Use of MedChemExpress (MCE) Aprepitant

All Neurokinin Receptor Isoforms

All HIV Isoforms

All Antibiotic Isoforms

Biological Activity

Chemical Information

Publications (13)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Aprepitant Related Classifications

Cat. No.: HY-10052