2015年6月1日星期一

Netupitant|neurokinin-1 receptor antagonist|DC Chemicals

Netupitant|neurokinin-1 receptor antagonist|DC Chemicals
Netupitant is a highly potent and selective, orally active neurokinin-1 receptor antagonist with Ki of 0.95 nM.

Catlog: DC8100| Product name: Netupitant| Cas: 290297-26-6| Other names: Netupitant (Ro 67-31898)| Molecule Formula: C30H32F6N4O| MW: 578.59. Purity: >98%

Price: 100mg: 1100 USD; 250mg: 2200 USD; 1000mg: 3500 USD

Netupitant is a highly potent and selective, orally active neurokinin-1 receptor antagonist with Ki of 0.95 nM.
IC50 value: 0.95 nM (Ki)
in vitro: Netupitant also dose-dependently inhibited the SP response as expected from an NK1 receptor antagonist. Importantly, when both palonosetron and netupitant were present, they exhibited an enhanced inhibition of the SP response compared to either of the two antagonists alone.
in vivo: In mice the intrathecal injection of SP elicited the typical scratching, biting and licking response that was dose-dependently inhibited by Netupitant given intraperitoneally in the 1-10mg/kg dose range. In gerbils, foot tapping behavior evoked by the intracerebroventricular injection of a NK(1) agonist was dose-dependently counteracted by Netupitant given intraperitoneally (ID(50) 1.5mg/kg) or orally (ID(50) 0.5mg/kg).

For research and scientific purpose only, not for human use.

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