中文名:奈妥吡坦
英文名:Netupitant
纯度:Moligand™,≥99%
货号:N413162
Cas号:290297-26-6
存储温度:-20°C储存
运输条件:超低温运输
产品介绍:
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
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关键字: KZVBBVPCVQEVQK-UHFFFAOYSA-N ; UNII-7732P08TIR ; NSC68808 ; 1,3,3-Tetraethoxypropane
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