Aprepitant

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.
Targets
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 NXnyOYszTnWwY4Tpc44h[XO|YYm= M{[xOGRqe3CuYXPlcYVvfCCxZjDbNVI2UV2VUDDmdo9uKGi3bXHuJG5MOSC{ZXPldJRweiCneIDy[ZN{\WRiaX6gR2hQKGOnbHzzMEBKSzVyPUnlMVA2KM7:TR?= MYWxO|czOzNyMB?=
HEK293 cell M4\wO2Z2dmO2aX;uJIF{e2G7 MYnEbZNxdGGlZX3lcpQhd2ZiW{GyOWleNXO3YoP0ZY5k\SCSIH\yc40h\2W{YnnsJG5MOSC{ZXPldJRweiCneIDy[ZN{\WRiaX6gTGVMOjl|IHPlcIwhdWWvYoLhcoV{KGmwY4XiZZRm\CCob4KgN|AhdWmwczDifUBtcXG3aXSgd4NqdnSrbHzheIlwdiClb4XueIlv\yCvZYToc4QtKEmFNUC9PYUuODVizszN NEC5SmwzPjB2OEiwNC=>
HEK293 cell M{TiU2Z2dmO2aX;uJIF{e2G7 M3\LOm5wdmOxbYDleIl1cX[nIHnubIljcXSrb36gc4Yhf2muZDD0fZBmKGi3bXHuJG5MOSC{ZXPldJRweiCneIDy[ZN{\WRiaX6gTGVMOjl|IHPlcIx{KGG|c3Xzd4VlKGG|IHTlZ5Jm[XOnIHnuJHNROS2rbnT1Z4VlKFt|SG3JVEBi[2O3bYXsZZRqd25iYX\0[ZIhOjBibXnudy=> M3fIUlIzPTd2OUez

... 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

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 individually and in order:
5% DMSO+corn oil
13mg/mL

* 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
Formula

C23H21F7N4O3

CAS No. 170729-80-3
Storage powder
Synonyms MK-0869, L-754030

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03035838 Not yet recruiting Traumatic Brain Injury Arun Gupta|Cambridge University Hospitals NHS Foundation Trust|University of Cambridge March 2017 Early Phase 1
NCT02989467 Not yet recruiting Healthy Mayo Clinic December 2016 Phase 1
NCT02909478 Not yet recruiting Chemotherapy-induced Nausea and Vomiting|Colorectal Cancer Sun Yat-sen University December 2016 Phase 3
NCT02770378 Recruiting Glioblastoma University of Ulm|Reliable Cancer Therapies|Anticancer Fund, Belgium November 2016 Phase 1
NCT02979548 Recruiting Chemotherapy Induced Vomiting|Acute Myeloid Leukemia Dr Atul Sharma|All India Institute of Medical Sciences, New Delhi November 2016 Phase 3
NCT02939287 Not yet recruiting Nausea|Vomiting Rush University Medical Center November 2016 Phase 3

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID