Aprepitant
Based on 13 publication(s) in Google Scholar
Aprepitant (MK-0869) is a selective and high-affinity neurokinin 1 receptor antagonist with a Kd of 86 pM.
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- Pureza: 99.82%
- No. CAS: 170729-80-3
- Fòrmula: C23H21F7N4O3
- Peso molecular:534.43
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Aprepitant
More- Cell Death Dis. 2023 Jun 29;14(6):384. [Abstract]
- Cell Death Dis. 2022 Jan 10;13(1):41. [Abstract]
- Liver Int. 2024 Jul;44(7):1651-1667. [Abstract]
- Sci Rep. 2026 Feb 9;16(1):7851. [Abstract]
- Sci Rep. 2025 Oct 21;15(1):36723. [Abstract]
- Korean J Pain. 2022 Apr 1;35(2):173-182. [Abstract]
- Front Pain Res. 2021 Jul 1:2:672711. [Abstract]
- 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. 2021 May 14:2021:6681815. [Abstract]
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Apoptosis Analysis
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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Actividad biológica
Kd: 86 pM (Neurokinin 1 receptor)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
18.3 μM
Compound: Aprepitant
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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
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[PMID: 34236855] |
| A549 | IC50 |
18.3 μM
Compound: Aprepitant
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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
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[PMID: 34236855] |
| CHO | IC50 |
0.09 nM
Compound: 1, Aprepitant
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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
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[PMID: 16824752] |
| CHO | IC50 |
0.09 nM
Compound: 1, Aprepitant
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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
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[PMID: 16831551] |
| CHO | IC50 |
0.09 nM
Compound: 1, aprepitant
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Displacement of [125I]SP from human NK1 receptor expressed in CHO cells
Displacement of [125I]SP from human NK1 receptor expressed in CHO cells
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[PMID: 17723300] |
| CHO | IC50 |
0.09 nM
Compound: 17
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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
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[PMID: 9804700] |
| HEK293 | IC50 |
0.09 nM
Compound: 1
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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
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[PMID: 26048800] |
| Kelly | IC50 |
15.1 μM
Compound: Aprepitant
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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
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[PMID: 38086194] |
| MRC5 | IC50 |
28.9 μM
Compound: Aprepitant
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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
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[PMID: 34236855] |
| TERT-RPE1 | IC50 |
176.3 μM
Compound: Aprepitant
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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
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[PMID: 38086194] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 170729-80-3
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Appearance Solid
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Peso molecular 534.43
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Fòrmula C23H21F7N4O3
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Color White to off-white
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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
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Synonyms
MK-0869; MK-869; L-754030
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)
Publications (13)
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Journal Impact Factor
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Most Recent
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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.
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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.
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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
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
2021 Jul 1:2:672711. PMID: 35295455 -
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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
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline 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.
Add each solvent one by one: Corn Oil
Solubility: 10 mg/mL (18.71 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
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.
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.
Pureza y Documentación
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Ficha de datos (282 KB)
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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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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]
Complete Stock Solution Preparation Table
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.
| 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 |
Aprepitant Related Classifications
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