| 中文名称: | Vofopitant | ||||
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| 英文名称: | Vofopitant | ||||
| 别名: | (2S,3S)-N-[[2-methoxy-5-[5-(trifluoromethyl)tetrazol-1-yl]phenyl]methyl]-2-phenylpiperidin-3-amine | ||||
| CAS No: | 168266-90-8 | 分子式: | C21H23F3N6O | 分子量: | 432.44 |
| CAS No: | 168266-90-8 | ||||
| 分子式: | C21H23F3N6O | ||||
| 分子量: | 432.44 | ||||
基本信息
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产品编号：V10222 |
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产品名称：Vofopitant |
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CAS: |
168266-90-8 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
六个月 |
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分子量： |
432.44 |
-20℃ |
一个月 |
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化学名： |
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Solubility (25°C) |
体外 |
DMSO |
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Ethanol |
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Water |
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体内（现配现用） |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
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生物活性
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产品描述 |
一种有效的 NK1 receptor 拮抗剂，对人，大鼠和雪貂的 NK1 receptor 的 pKi 值分别为 10.6，9.5 和 9.8。 |
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靶点/IC50 |
pKi:10.6 (Human NK1 receptor),9.5 (Rat NK1 receptor),9.8 (Ferret NK1 receptor) |
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体外研究 |
Vofopitant is potent tachykinin NK1 receptor antagonist,with pKis of 10.6,9.5,and 9.8 for human,rat and ferret NK1 receptor,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 NK2 and NK3,with pIC50 of <5.0.GR205171 (300µM) potentiates the effects of paroxetine on cortical [5-HT]ext,and inhibits paroxetine-induced increase in [5-HT]ext in the dorsal raphe nucleus. |
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体内研究 |
Vofopitant (GR205171,30mg/kg,s.c.) increases the number of choices of the 25-s delayed reward in a T-maze.Vofopitant (GR205171,30mg/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. |
推荐实验方法(仅供参考)
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激酶实验： |
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Tachykinin NK1 receptor binding assays are carried out in an assay volume of 200μL,consisting of 50μL of wash buffer (containing HEPES (50mM) and MnC12 (3mM),pH 7.4) or test compound (Vofopitant),100μL membrane suspension (3-5μg of protein) in HEPES assay buffer (composition as above,but containing bacitracin,80μg/mL],leupeptin, 8μg/mL],phosphoramidon,2μM and bovine serum albumin, 0.04%) and 50μL of [3H]substance P (0.7-1.0nM final concentration).The incubation is carried out at room temperature for 40 min.Non-specific binding is defined by the addition of CP-99,994 (1μM). |
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动物实验: |
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Effect of NK1 receptor antagonists administered i.p.on cortical [5-HT]ext of wild-type mice.Following collection of four baseline dialysate samples,freely moving wild-type mice are administered with either the vehicle or various NK1 receptor antagonists,Vofopitant (30mg/kg;i.p.) or L733060 (40mg/kg; i.p.).Dialysate samples are collected for a 0-120 min post treatment period. |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
