Netupitant - 2mM in DMSO, high purity , CAS No.290297-26-6

Item Number

N423021

• Synonyms: Netupitant | 290297-26-6 | 2-[3,5-bis(trifluoromethyl)phenyl]-N,2-dimethyl-N-[4-(2-methylphenyl)-6-(4-methylpiperazin-1-yl)pyridin-3-yl]propanamide | 2-(3,5-bis(trifluoromethyl)phenyl)-N,2-dimethyl-N-(6-(4-methylpiperazin-1-yl)-4-(o-tolyl)pyridin-3-yl)propanami
• Specifications & Purity: Moligand™, 2mM in DMSO
• Biochemical and Physiological Mechanisms: Netupitant (CID6451149) is a selective neurokinin 1 (NK1) receptor antagonist with potential antiemetic activity.
• Storage Temp: Store at -80°C
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™

Product Description

Information

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

Targets

Neurokinin-1 receptor

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.

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.

Cell Research(from reference)

Cell lines：NG108-15 cells 

Concentrations：1, 3, 10, 30 nM 

Incubation Time：1 h