产品信息
抗原名称
Neurokinin-1 receptor
商品描述
Netupitant is a selective <b>neurokinin 1 (NK1) receptor</b> antagonist with potential antiemetic activity.
分子量
578.59
纯度
98%
可溶性
DMSO : 9.09 mg/mL (15.71 mM; ultrasonic and warming and heat to 60°C)
外观
White powder
In vitro(体外研究)
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(体内研究)
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.
背景
别名
奈妥吡坦
分子式
C30H32F6N4O
CAS号
290297-26-6
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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