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Vofopitant
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Vofopitant图片
CAS NO:168266-90-8
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
GR 205171
产品介绍
Vofopitant 是一种有效的NK1receptor拮抗剂,对人,大鼠和雪貂的 NK1receptor 的pKi值分别为 10.6,9.5 和 9.8。
生物活性

Vofopitant is potenttachykinin NK1receptorantagonist, withpKis of 10.6, 9.5, and 9.8 for human, rat and ferret NK1receptor, respectively.

IC50& Target

pKi: 10.6 (Human NK1receptor), 9.5 (Rat NK1receptor), 9.8 (Ferret NK1receptor)[1]

体外研究
(In Vitro)

Vofopitant is potent tachykinin NK1receptor antagonist, with pKis of 10.6, 9.5, and 9.8 for human, rat and ferret NK1receptor, respectively. Vofopitant less potently inhibits rat 5-HT1A, bovine 5-HT1D, rat 5-HT2A, rat Histamine H1, guinea-pig Histamine H2 and rat Ca2+channel, with pKis of 6.3, 6.6, 6.5, 6.5, 6.6, and 5.6, respectively. Vofopitant shows negligible affinity at NK2and NK3, with pIC50of<5.0[1]. GR205171 (300 μM) potentiates the effects of paroxetine on cortical [5-HT]ext, and inhibits paroxetine-induced increase in [5-HT]ext in the dorsal raphe nucleus[3].

体内研究
(In Vivo)

Vofopitant (GR205171, 30 mg/kg, s.c.) increases the number of choices of the 25-s delayed reward in a T-maze[2]. Vofopitant (GR205171, 30 mg/kg, i.p.) increases the extracellular 5-HT levels in the frontal cortex of paroxetine-treated wild-type mice, rather than in wild-type mice and paroxetine-treated NK1 receptor knockout mice[3].

Clinical Trial
分子量

432.44

性状

Solid

Formula

C21H23F3N6O

CAS 号

168266-90-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month