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Aprepitant (MK-0869)

Name: Aprepitant (MK-0869)
Brand: Selleck Chemicals
SKU: S1189
Rating: 5 (20 reviews)

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.

CAS No. 170729-80-3

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

Purity & Quality Control

Choose Selective Neurokinin Receptor Inhibitors

Related Compound Libraries

Biological Activity

Description

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=>

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]

Protocol (from reference)

References

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. Click to purchase: Corn Oil	13mg/mL

Chemical Information

Molecular Weight	534.43
Formula	C₂₃H₂₁F₇N₄O₃
CAS No.	170729-80-3
Storage	3 years	-20°C	powder
Storage	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

Download Aprepitant (MK-0869) SDF

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:μL Number of animals:

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% DMSO + % + % Tween 80 + % ddH₂O

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

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.

Handling Instructions

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