Home Neuronal Signaling Neurokinin Receptor antagonist Netupitant For research use only.

Netupitant

Synonyms: CID6451149, CID 6451149, CID-6451149

Netupitant (CID6451149) is a selective neurokinin 1 (NK1) receptor antagonist with potential antiemetic activity.

Netupitant Chemical Structure

Netupitant Chemical Structure

CAS No. 290297-26-6

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Biological Activity

Description Netupitant (CID6451149) is a selective neurokinin 1 (NK1) receptor antagonist with potential antiemetic activity.
Targets
Neurokinin-1 receptor [1]
In vitro
In vitro In CHO NK1 cells, Netupitant concentration-dependently antagonizes the stimulatory effects of substance P (SP) showing insurmountable antagonism (pKB 8.87). In cells expressing NK2 or NK3 receptors, Netupitant is inactive[1].
Cell Research Cell lines NG108-15 cells
Concentrations 1, 3, 10, 30 nM
Incubation Time 1 h
Method

cells are preincubated for 1 h at 37℃ with either growth media alone(control) or media containing antagonists. Antagonist concentrations are at least 30-fold the Kd value to ensure receptor saturation. After preincubation, antagonists are removed and cells are rinsed with growth media alone for an additional hour to allow for dissociation of antagonists still bound to receptor.Cell media are then replaced with isosmotic HEPES buffer (pH 7.4, 20 mM) containing NaCl (130 mM), KCl (2 mM), MgCl2 (1 mM) CaCl2 (2 mM), Fluo-4 acetoxymethyl (AM) ester (2 mM), pluronic acid (0.04%) and SP at various concentrations in the 3 nM to 1 mM range. The final incubation lasted for 1 h at 37 ℃. Pluronic acid is added as a nonionic surfactant to sequester the AM ester molecules into micelles for cellular uptake.
In Vivo
In vivo Netupitant behaves as a brain penetrant, orally active, potent and selective NK1 antagonist. In mice the intrathecal injection of SP elicited the typical scratching, biting and licking response that is dose-dependently inhibited by Netupitant given intraperitoneally in the 1-10 mg/kg dose range. In gerbils, foot tapping behavior evoked by the intracerebroventricular injection of a NK1 agonist is dose-dependently counteracted by Netupitant given intraperitoneally (ID50 1.5 mg/kg) or orally (ID50 0.5 mg/kg). In time course experiments in gerbils Netupitant displayed long lasting effects[1].
Animal Research Animal Models Male Swiss mice
Dosages 1 and 10 mg/kg
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04486157 Completed
Healthy
HK inno.N Corporation
 March 18 2021 Phase 1
NCT03204279 Completed
Chemotherapy-induced Nausea and Vomiting (CINV)
Helsinn Healthcare SA
 August 31 2017 Phase 2

Chemical Information & Solubility

Molecular Weight 578.59 Formula

C30H32F6N4O
CAS No. 290297-26-6 SDF Download Netupitant SDF
Smiles CC1=CC=CC=C1C2=CC(=NC=C2N(C)C(=O)C(C)(C)C3=CC(=CC(=C3)C(F)(F)F)C(F)(F)F)N4CCN(CC4)C
Storage (From the date of receipt)

In vitro
Batch:

Ethanol : 100 mg/mL

DMSO : 2 mg/mL ( (3.45 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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In vivo
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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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