アプレピタント (Synonyms: Aprepitant; MK-0869; MK-869; L-754030)

Name: Aprepitant
Brand: MedChemExpress
SKU: HY-10052
Rating: 5.0 (13 reviews)

製品番号: HY-10052 純度: 99.82%: Data Sheet SDS COA 取扱説明書
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Technical Support

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

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CAS 番号 : 170729-80-3

容量	価格（税別）	在庫状況	数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 78	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 78	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$66	在庫あり	Estimated Time of Arrival: December 31
10 mg	$79	在庫あり	Estimated Time of Arrival: December 31
50 mg	$106	在庫あり	Estimated Time of Arrival: December 31
100 mg	$131	在庫あり	Estimated Time of Arrival: December 31
200 mg	$158	在庫あり	Estimated Time of Arrival: December 31
500 mg	$198	在庫あり	Estimated Time of Arrival: December 31
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カスタマーレビュー

Based on 13 publication(s) in Google Scholar

Other Forms of Aprepitant:

Aprepitant-d₄ 在庫あり
Aprepitant (Standard) 在庫あり
Aprepitant-¹³C₂,d₂ (Major) お問い合わせ

顧客検証

Apoptosis Analysis

Cell Proliferation/Viability Assay

: 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.

: 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.

Neurokinin Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

NK1R NK2R NK3R

HIV アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

HIV HIV-1 HIV-2

Antibiotic アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

Aminoglycoside Glycopeptide Lipopeptide Macrolide Oxazolidinone Quinolone Tetracycline β-lactam

生物活性
プロトコル
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

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]

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]

体外実験

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.

体内実験

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.

臨床実験

分子量

534.43

分子式

C₂₃H₂₁F₇N₄O₃

CAS 番号

170729-80-3

Appearance

Solid

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, protect from light

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

溶剤 & 溶解度

体外:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Molarity Calculator
Dilution Calculator

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

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.

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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

純度とドキュメンテーション

純度: 99.82%

Select Batch:

データシート (282 KB) SDS (393 KB)

COA (252 KB) HNMR (289 KB) RP-HPLC (266 KB) LCMS (89 KB)

取扱説明書 (2659 KB)

参考文献

[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]

細胞実験 ^[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) はこれらの方法の精度を確認していません。こちらは参照専用です。
動物実験 ^[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) はこれらの方法の精度を確認していません。こちらは参照専用です。
参考文献	[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

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

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

Help & FAQs

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Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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アプレピタント (Synonyms: Aprepitant; MK-0869; MK-869; L-754030)

カスタマーレビュー

Other Forms of Aprepitant:

顧客検証

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純度とドキュメンテーション

参考文献

カスタマーレビュー

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Aprepitant Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

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アプレピタント (Synonyms: Aprepitant; MK-0869; MK-869; L-754030)

カスタマーレビュー

Other Forms of Aprepitant:

アプレピタント 関連抗体

顧客検証

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

Neurokinin Receptor アイソフォーム固有の製品をすべて表示:

HIV アイソフォーム固有の製品をすべて表示:

Antibiotic アイソフォーム固有の製品をすべて表示:

生物活性

プロトコル

純度とドキュメンテーション

参考文献

カスタマーレビュー

アプレピタント 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Aprepitant Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

最近チェックした製品:

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アプレピタント関連抗体

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