Aprepitant (MK-0869)

Catalog No.S1189 Synonyms: L-754030

For research use only.

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.

Aprepitant (MK-0869) Chemical Structure

CAS No. 170729-80-3

Selleck's Aprepitant (MK-0869) has been cited by 20 publications

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.
Targets
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 NW\tSXg2TnWwY4Tpc44h[XO|YYm= MXvEbZNxdGGlZX3lcpQhd2ZiW{GyOWleW1BiZoLvcUBpfW2jbjDOT|EhemWlZYD0c5Ih\XiycnXzd4VlKGmwIFPIU{Bk\WyuczygTWM2OD17ZT2wOUDPxE1? Mnj6NVc4OjN|MEC=
HEK293 cell MUjGeY5kfGmxbjDhd5NigQ>? MnfySIl{eGyjY3Xt[Y51KG:oIGuxNlVKZS2|dXLzeIFv[2ViUDDmdo9uKGencnLpcEBPUzFicnXj[ZB1d3JiZYjwdoV{e2WmIHnuJGhGUzJ7MzDj[YxtKG2nbXLyZY5meyCrbnP1ZoF1\WRiZn;yJFMxKG2rboOgZpkhdGmzdXnkJJNkcW62aXzsZZRqd25iY3;1cpRqdmdibXX0bI9lNCCLQ{WwQVlmNTB3IN88US=> MXyyOlA1QDhyMB?=
HEK293 cell M2XjSWZ2dmO2aX;uJIF{e2G7 NWC3PFhNVm:wY3;tdIV1cXSrdnWgbY5pcWKrdHnvckBw\iC5aXzkJJR6eGViaIXtZY4hVktzIILlZ4VxfG:{IHX4dJJme3OnZDDpckBJTUt{OUOgZ4VtdHNiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4hW1BzLXnu[JVk\WRiW{PIYWlRKGGlY4XteYxifGmxbjDh[pRmeiB{MDDtbY5{ NEXkWG4zOjV5NEm3Ny=>
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]

Protocol (from reference)

Solubility (25°C)

In vitro

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.

13mg/mL

Chemical Information

Molecular Weight 534.43
Formula

C23H21F7N4O3

CAS No. 170729-80-3
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Molarity Calculator

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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 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 LLC|State University of New York - Upstate Medical University April 2015 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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.

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