Aprepitant
Catalog No.S1189 Synonyms: MK-0869, L-754030
Molecular Weight(MW): 534.43
Aprepitant is a potent and selective neurokinin-1 receptor antagonist with IC50 of 0.1 nM.
2 Customer Reviews
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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
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Biological Activity
| Description | Aprepitant is a potent and selective neurokinin-1 receptor antagonist with IC50 of 0.1 nM. | ||||||||||||||||||||||||||||||
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| 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] |
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| Cell Data |
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| 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 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 |
* 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 |
| in solvent | |
| Synonyms | MK-0869, L-754030 |
Bio Calculators
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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 | October 2019 | Early Phase 1 |
| NCT03035838 | Not yet recruiting | Traumatic Brain Injury | Arun Gupta|Cambridge University Hospitals NHS Foundation Trust|University of Cambridge | October 2019 | Early Phase 1 |
| NCT03808805 | Not yet recruiting | Myeloproliferative Disorder|Aquagenic Pruritus | University Hospital Brest | March 1 2019 | Phase 3 |
| NCT03876938 | Recruiting | Antiemetic for Highly Emetogenic Chemotherapy | Mahidol University | March 1 2019 | Phase 3 |
| NCT03586817 | Recruiting | Nausea and Vomiting Postoperative | Hospital Federal de Bonsucesso | March 2 2019 | Phase 4 |
| NCT03586817 | Recruiting | Nausea and Vomiting Postoperative | Hospital Federal de Bonsucesso | March 2 2019 | Phase 4 |
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