For research use only.

Catalog No.S4654 Synonyms: CID6451149, CID 6451149, CID-6451149

1 publication

Netupitant Chemical Structure

CAS No. 290297-26-6

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

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Selleck's Netupitant has been cited by 1 publication

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Choose Selective Neurokinin Receptor Inhibitors

Biological Activity

Description Netupitant (CID6451149) is a selective neurokinin 1 (NK1) receptor antagonist with potential antiemetic activity.
Neurokinin-1 receptor [1]
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].

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].


Cell Research:


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  • 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.

    (Only for Reference)
Animal Research:


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  • Animal Models: Male Swiss mice
  • Dosages: 1 and 10 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro Ethanol 100 mg/mL (172.83 mM)
DMSO 2 mg/mL (3.45 mM)
Water Insoluble

* 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 578.59


CAS No. 290297-26-6
Storage powder
in solvent
Synonyms CID6451149, CID 6451149, CID-6451149
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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID