Aprepitant (MK-0869)

For research use only.

Catalog No.S1189 Synonyms: L-754030

18 publications

Aprepitant (MK-0869) Chemical Structure

CAS No. 170729-80-3

Aprepitant (MK-0869, L-754030) is a potent and selective neurokinin-1 receptor antagonist with IC50 of 0.1 nM. Aprepitant reduces levels of pro-inflammatory cytokines including G-CSF, IL-6, IL-8 and TNFα. Aprepitant inhibits HIV infection of human macrophages.

Selleck's Aprepitant (MK-0869) has been cited by 18 publications

2 Customer Reviews

  • HepT1, HepG2, and HuH6 cells were treated with increasing doses of aprepitant or SP [100 nM] and Western blot analysis was performed for the apoptotic markers PARP, Caspase-3, and BID.

    J Hepatol, 2014, 60(5):985-94.. Aprepitant (MK-0869) purchased from Selleck.

  • The combination of Aprepitant and select shRNAs enhances hypoxia tolerance in kidney epithelial cells. HK-2 cells expressing shRNA targeting (a) C2ORF42 and (b) RHOB were treated with the indicated concentrations of Aprepitant and exposed to ischemic conditions for 48 h. For each dose of the drug, the numbers of cells remaining after treatment were analyzed as a percent of cells incubated under normoxic conditions. For each shRNA, the results are shown in comparison with those for vector-transduced HK-2 cells, which were treated in parallel. (c) Caspase activity following 40 h of ischemia was measured in HK-2 cells, modified or treated as indicated. Error bars for all panels indicate S.D. of three independent experiments. The asterisks indicate a significant (P<0.05, unless otherwise indicated in panel c) difference comparing the indicated treatment goups

    Cell Death Differ, 2016, 23(4):608-15. Aprepitant (MK-0869) purchased from Selleck.

Purity & Quality Control

Choose Selective Neurokinin Receptor Inhibitors

Biological Activity

Description Aprepitant (MK-0869, L-754030) is a potent and selective neurokinin-1 receptor antagonist with IC50 of 0.1 nM. Aprepitant reduces levels of pro-inflammatory cytokines including G-CSF, IL-6, IL-8 and TNFα. Aprepitant inhibits HIV infection of human macrophages.
G-CSF [3]
IL-6 [3]
IL-8 [3]
TNFα [3]
Neurokinin-1 receptor [1]
(Cell-free assay)
0.1 nM
In vitro

Aprepitant antagonizes the effects of substance P by binding to NK-1 receptors primarily in the CNS, but also in the periphery. Aprepitant, at concentrations of 0.1 nM displaces 50% of substance P from hNK1 receptors transfected in CHO or COS cells. In radioligand binding assays, Aprepitant is 3000-fold selective for the human cloned NK1 receptor versus the human cloned NK3 receptor and >50,000-fold selective over the human cloned NK2 receptor. In a range of assays at other human cloned G–protein coupled receptors, Aprepitant retains >50,000-fold selectivity for the human cloned NK1 receptor. Aprepitant is inactive in human monoamine oxidase A and B assays and at human serotonin 5–HT1A, 5–HT2A, 5–HT2c, 5–HT3, 5–HT5, 5–HT6, and 5–HT7 receptors (IC50>3 μM). In the PANLABS panel of radioligand binding screens using native animal tissues, Aprepitant inhibits [3H]substance P binding to native NK1 receptors in rat submaxillary gland; there are no significant interactions of Aprepitant with any other native animal G–protein coupled receptors or ion channels examined in the PANLABS screen. Aprepitant is inactive in monoamine uptake site (NE, 5–HT, DA) counterscreens using human and animal tissues (IC50> 3 μM) [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293 cell NYXSPHpYTnWwY4Tpc44h[XO|YYm= MVPEbZNxdGGlZX3lcpQhd2ZiW{GyOWleNXO3YoP0ZY5k\SCSIH\yc40h\2W{YnnsJG5MOSC{ZXPldJRweiCneIDy[ZN{\WRiaX6gTGVMOjl|IHPlcIwhdWWvYoLhcoV{KGmwY4XiZZRm\CCob4KgN|AhdWmwczDifUBtcXG3aXSgd4NqdnSrbHzheIlwdiClb4XueIlv\yCvZYToc4QtKEmFNUC9PYUuODVizszN Mo\yNlYxPDh6MEC=
HEK293 cell Mk\WSpVv[3Srb36gZZN{[Xl? MVTOc45kd22yZYTpeIl3\SCrbnjpZol1cW:wIH;mJJdqdGRidInw[UBpfW2jbjDOT|EhemWlZYD0c5Ih\XiycnXzd4VlKGmwIFjFT|I6OyClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDTVFEucW6mdXPl[EBcO0ifSWCgZYNkfW23bHH0bY9vKGGodHXyJFIxKG2rboO= MmrJNlI2PzR7N{O=

... Click to View More Cell Line Experimental Data

In vivo

Aprepitant crosses the blood–brain barrier and occupied NK-1 receptors in the brain. Aprepitant has been shown to inhibit both acute and delayed emesis induced by cytotoxic chemotherapeutic such as cisplatin by blocking substance P. Aprepitant (3 mg/kg i.v. or p.o.) inhibits the emetic response to cisplatin (10 mg/kg i.v.). The anti-emetic protection afforded by Aprepitant (0.1 mg/kg i.v.) is enhanced by combined treatment with either dexamethasone (20 mg/kg i.v.) or the 5–HT3 receptor antagonist ondansetron (0.1 mg/kg i.v.). In a model of acute and delayed emesis, ferrets are dosed with cisplatin (5 mg/kg i.p.) and the retching and vomiting response recorded for 72 h. Pretreatment with Aprepitant (4–16 mg/kg p.o.) dose-dependently inhibits the emetic response to cisplatin. Once daily treatment with Aprepitant (2 and 4 mg/kg p.o.) completely prevents retching and vomiting in all ferrets tested. Further when daily dosing began at 24 h after cisplatin injection, when the acute phase of emesis had already become established, Aprepitant (4 mg/kg p.o. at 24 and 48 h after cisplatin) prevents retching and vomiting in three out of four ferrets. [1] Aprepitant also plays a key part in transmission of pain impulses from the peripheral receptors to the CNS and is involved in various behavioural, neurochemical and cardiovascular responses to stress. [2]


Solubility (25°C)

In vitro DMSO 107 mg/mL (200.21 mM)
Water Insoluble
Ethanol ''15 mg/mL
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+corn oil
For best results, use promptly after mixing.

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 534.43


CAS No. 170729-80-3
Storage powder
in solvent
Synonyms L-754030
Smiles CC(C1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)OC2C(N(CCO2)CC3=NNC(=O)N3)C4=CC=C(C=C4)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04075955 Completed Drug: Zyprexa® (OLANZapine 5MG)|Drug: Emend® (Aprepitant) Chemotherapy-induced Nausea and Vomiting CR-CSSS Champlain-Charles-Le Moyne April 29 2019 Phase 3
NCT03683225 Unknown status Combination Product: CTC-413 Idiopathic Parkinson Disease Chase Therapeutics Corporation April 1 2019 Phase 2
NCT02407600 Unknown status Drug: FOSAPREPITANT (Emend)|Drug: Placebo Non-small Cell Lung Cancer|Vomiting|Nausea|Emesis Ajeet Gajra|Merck Sharp & Dohme Corp.|State University of New York - Upstate Medical University April 2015 Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field
Tags: buy Aprepitant (MK-0869) | Aprepitant (MK-0869) ic50 | Aprepitant (MK-0869) price | Aprepitant (MK-0869) cost | Aprepitant (MK-0869) solubility dmso | Aprepitant (MK-0869) purchase | Aprepitant (MK-0869) manufacturer | Aprepitant (MK-0869) research buy | Aprepitant (MK-0869) order | Aprepitant (MK-0869) mouse | Aprepitant (MK-0869) chemical structure | Aprepitant (MK-0869) mw | Aprepitant (MK-0869) molecular weight | Aprepitant (MK-0869) datasheet | Aprepitant (MK-0869) supplier | Aprepitant (MK-0869) in vitro | Aprepitant (MK-0869) cell line | Aprepitant (MK-0869) concentration | Aprepitant (MK-0869) nmr
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID