Vofopitant (GR 205171)
(Synonyms: GR 205171) 目录号 : GC33747
Vofopitant (GR 205171) 是有效的速激肽 NK1 受体拮抗剂，对人、大鼠和雪貂 NK1 受体的 pKis 分别为 10.6、9.5 和 9.8。
Cas No.:168266-90-8
Sample solution is provided at 25 µL, 10mM.
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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 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[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].
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].
[1]. Gardner CJ, et al. GR205171: a novel antagonist with high affinity for the tachykinin NK1 receptor, and potent broad-spectrum anti-emetic activity. Regul Pept. 1996 Aug 27;65(1):45-53. [2]. Loiseau F, et al. Antidepressant-like effects of agomelatine, melatonin and the NK1 receptor antagonist GR205171 in impulsive-related behaviour in rats. Psychopharmacology (Berl). 2005 Oct;182(1):24-32. Epub 2005 Sep 29. [3]. Guiard BP, et al. Blockade of substance P (neurokinin 1) receptors enhances extracellular serotonin when combined with a selective serotonin reuptake inhibitor: an in vivo microdialysis study in mice. J Neurochem. 2004 Apr;89(1):54-63.
Kinase experiment: | Tachykinin NK1 receptor binding assays are carried out in an assay volume of 200 μL, consisting of 50 μL of wash buffer (containing HEPES (50 mM) and MnC12 (3 mM), pH 7.4) or test compound (Vofopitant), 100 μL membrane suspension (3-5 μg of protein) in HEPES assay buffer (composition as above, but containing bacitracin, 80 μg/mL], leupeptin, 8 μg/mL], phosphoramidon, 2 μM and bovine serum albumin, 0.04%) and 50 μL of [3H]substance P (0.7-1.0 nM 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 (1 μM)[1]. |
Animal experiment: | 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 (30 mg/kg; i.p.) or L733060 (40 mg/kg; i.p.). Dialysate samples are collected for a 0-120 min post-treatment period[3]. |
References: [1]. Gardner CJ, et al. GR205171: a novel antagonist with high affinity for the tachykinin NK1 receptor, and potent broad-spectrum anti-emetic activity. Regul Pept. 1996 Aug 27;65(1):45-53. | |
| Cas No. | 168266-90-8 | SDF | |
| 别名 | GR 205171 | ||
| Canonical SMILES | COC1=C(CN[C@@H]2[C@H](C3=CC=CC=C3)NCCC2)C=C(N4C(C(F)(F)F)=NN=N4)C=C1 | ||
| 分子式 | C21H23F3N6O | 分子量 | 432.44 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 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。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3125 mL | 11.5623 mL | 23.1246 mL |
| 5 mM | 0.4625 mL | 2.3125 mL | 4.6249 mL |
| 10 mM | 0.2312 mL | 1.1562 mL | 2.3125 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
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