For research use only.

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

16 publications

Aprepitant 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.

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Selleck's Aprepitant has been cited by 16 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 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 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
CHO cells NH7QPFBHfW6ldHnvckBie3OjeR?= M{WwemRqe3CuYXPlcYVvfCCxZjDbNVI2UV2VUDDmdo9uKGi3bXHuJG5MOSC{ZXPldJRweiCneIDy[ZN{\WRiaX6gR2hQKGOnbHzzMEBKSzVyPUnlMVA2KM7:TR?= MmXsNVc4OjN|MEC=
HEK293 cell NXq1O4s1TnWwY4Tpc44h[XO|YYm= NGnGUXpFcXOybHHj[Y1mdnRib3[gX|EzPUmfLYP1ZpN1[W6lZTDQJIZzd21iZ3XyZoltKE6NMTDy[YNmeHSxcjDlfJBz\XO|ZXSgbY4hUEWNMkmzJINmdGxibXXtZpJidmW|IHnuZ5Vj[XSnZDDmc5IhOzBibXnud{BjgSCuaYH1bYQhe2OrboTpcIxifGmxbjDjc5VvfGmwZzDt[ZRpd2RuIFnDOVA:QWVvMEWg{txO M1jiSFI3ODR6OECw
HEK293 cell M4jEPWZ2dmO2aX;uJIF{e2G7 MoLHUo9v[2:vcHX0bZRqfmViaX7obYJqfGmxbjDv[kB4cWymIIT5dIUhcHWvYX6gUmsyKHKnY3XweI9zKGW6cILld5Nm\CCrbjDISWszQTNiY3XscJMh[XO|ZYPz[YQh[XNiZHXjdoVie2ViaX6gV3AyNWmwZIXj[YQhYzOKXVnQJIFk[3WvdXzheIlwdiCjZoTldkAzOCCvaX7z M2jLS|IzPTd2OUez

... 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
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

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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 Recruiting Combination Product: CTC-413 Idiopathic Parkinson Disease Chase Therapeutics Corporation April 1 2019 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID