VOFOPITANT
VOFOPITANT 性质
| 沸点 | 542.5±60.0 °C(Predicted) |
|---|---|
| 密度 | 1.39±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 溶于二甲基亚砜 |
| 酸度系数(pKa) | 9.13±0.10(Predicted) |
| CAS 数据库 | 168266-90-8 |
VOFOPITANT 用途与合成方法
pKi: 10.6 (Human NK 1 receptor), 9.5 (Rat NK 1 receptor), 9.8 (Ferret NK 1 receptor)
Vofopitant is potent tachykinin NK 1 receptor antagonist, with pK i s of 10.6, 9.5, and 9.8 for human, rat and ferret NK 1 receptor, respectively. Vofopitant less potently inhibits rat 5-HT1A, bovine 5-HT1D, rat 5-HT2A, rat Histamine H1, guinea-pig Histamine H2 and rat Ca 2+ channel, with pK i s of 6.3, 6.6, 6.5, 6.5, 6.6, and 5.6, respectively. Vofopitant shows negligible affinity at NK 2 and NK 3 , with pIC 50 of <5.0. 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.
Vofopitant (GR205171, 30 mg/kg, s.c.) increases the number of choices of the 25-s delayed reward in a T-maze. 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.
VOFOPITANT 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024-04-30 | HY-12142 | 1 mg | 1300 | ||
| 2024-04-30 | HY-12142 | VOFOPITANT | 168266-90-8 | 5mg | 3000 |
