Netupitant

Catalog No.S4654 Batch:S465401

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Technical Data

Formula

C30H32F6N4O
Molecular Weight 578.59 CAS No. 290297-26-6
Solubility (25°C)* In vitro Ethanol 100 mg/mL (172.83 mM)
DMSO 2 mg/mL (3.45 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 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].

Protocol (from reference)

Cell Assay:

[2]
  • 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.
Animal Study:

[1]
  • Animal Models

    Male Swiss mice

  • Dosages

    1 and 10 mg/kg

  • Administration

    i.p.

Selleck's Netupitant has been cited by 1 publication

Crystal structures of the human neurokinin 1 receptor in complex with clinically used antagonists. [ Nat Commun, 2019, 10(1):17] PubMed: 30604743

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.