Catalog No.S1189 Synonyms: MK-0869, L-754030

Aprepitant Chemical Structure

Molecular Weight(MW): 534.43

Aprepitant is a potent and selective neurokinin-1 receptor antagonist with IC50 of 0.1 nM.

Size Price Stock Quantity  
In DMSO USD 420 In stock
USD 120 In stock
USD 210 In stock
USD 370 In stock
USD 570 In stock
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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 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 purchased from Selleck.

Purity & Quality Control

Choose Selective Substance P Inhibitors

Biological Activity

Description Aprepitant is a potent and selective neurokinin-1 receptor antagonist with IC50 of 0.1 nM.
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
CHO cells MnzPSpVv[3Srb36gZZN{[Xl? NUPSdG5KTGm|cHzhZ4Vu\W62IH;mJHsyOjWLXWPQJIZzd21iaIXtZY4hVktzIILlZ4VxfG:{IHX4dJJme3OnZDDpckBEUE9iY3XscJMtKEmFNUC9PYUuODVizszN M4DZWlE4PzJ|M{Cw
HEK293 cell MV;GeY5kfGmxbjDhd5NigQ>? NH:4bIhFcXOybHHj[Y1mdnRib3[gX|EzPUmfLYP1ZpN1[W6lZTDQJIZzd21iZ3XyZoltKE6NMTDy[YNmeHSxcjDlfJBz\XO|ZXSgbY4hUEWNMkmzJINmdGxibXXtZpJidmW|IHnuZ5Vj[XSnZDDmc5IhOzBibXnud{BjgSCuaYH1bYQhe2OrboTpcIxifGmxbjDjc5VvfGmwZzDt[ZRpd2RuIFnDOVA:QWVvMEWg{txO M3L0bVI3ODR6OECw
HEK293 cell NXqyUG5ETnWwY4Tpc44h[XO|YYm= MXzOc45kd22yZYTpeIl3\SCrbnjpZol1cW:wIH;mJJdqdGRidInw[UBpfW2jbjDOT|EhemWlZYD0c5Ih\XiycnXzd4VlKGmwIFjFT|I6OyClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDTVFEucW6mdXPl[EBcO0ifSWCgZYNkfW23bHH0bY9vKGGodHXyJFIxKG2rboO= NEXkT|MzOjV5NEm3Ny=>

... 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)
Ethanol 15 mg/mL (28.06 mM)
Water Insoluble
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 MK-0869, L-754030

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00035295 Completed Major Depressive Disorder Merck Sharp & Dohme Corp. November 8 2001 Phase 3
NCT00818259 Terminated Chemotherapy-Induced Nausea and Vomiting Merck Sharp & Dohme Corp. February 5 2009 Phase 1
NCT02210195 Completed Cannabis Dependence|Alcohol Dependence|Cannabis Use Disorder|Alcohol Use Disorder The Scripps Research Institute|National Institute on Drug Abuse (NIDA) September 4 2014 Phase 2
NCT01649258 Terminated Breast Cancer|Nausea|Vomiting University of Southern California|National Cancer Institute (NCI) September 4 2012 Phase 1
NCT00048607 Completed Major Depressive Disorder Merck Sharp & Dohme Corp. July 30 2002 Phase 3
NCT00048594 Completed Major Depressive Disorder Merck Sharp & Dohme Corp. January 3 2002 Phase 3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID