Home Neuronal Signaling Neurokinin Receptor antagonist - HIV inhibitor - Interleukins inhibitor - TNF-alpha inhibitor - CSF-1R inhibitor Aprepitant For research use only.

Aprepitant

Synonyms: MK-0869, L-754030

Aprepitant 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 Chemical Structure

Aprepitant Chemical Structure

CAS: 170729-80-3

Selleck's Aprepitant has been cited by 37 publications

Purity & Quality Control

Batch: Purity: 99.91%
99.91

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CHO cells Function assay Displacement of [125I]SP from human NK1 receptor expressed in CHO cells, IC50=9e-05 μM 17723300
HEK293 cell Function assay Displacement of [125I]-substance P from gerbil NK1 receptor expressed in HEK293 cell membranes incubated for 30 mins by liquid scintillation counting method, IC50=9e-05 μM 26048800
HEK293 cell Function assay Noncompetitive inhibition of wild type human NK1 receptor expressed in HEK293 cells assessed as decrease in SP1-induced [3H]IP accumulation after 20 mins 22574973
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Biological Activity

Description Aprepitant 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
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]
In Vivo
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]
Animal Research Animal Models Male ferrets
Dosages 4, 8 or 16 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05755659 Recruiting Neoplasms Xijing Hospital July 15 2022 Not Applicable
NCT04075955 Completed Chemotherapy-induced Nausea and Vomiting CR-CSSS Champlain-Charles-Le Moyne April 29 2019 Phase 3
NCT03683225 Active not recruiting Idiopathic Parkinson Disease Chase Therapeutics Corporation April 1 2019 Phase 2
NCT03889366 Completed Healthy Nuformix Technologies Limited March 20 2019 Phase 1

Chemical lnformation & Solubility

Molecular Weight 534.43 Formula

C23H21F7N4O3
CAS No. 170729-80-3 SDF Download Aprepitant SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 107 mg/mL ( (200.21 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 15 mg/mL

Water : Insoluble


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In vivo
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