Vofopitant|168266-90-8|(GR 205171)-陌孚医药/Medlife

您当前的位置：

Vofopitant (Synonyms: GR 205171)

目录号: PL07732 纯度: ≥99%

CAS No. :168266-90-8

商品编号	规格	价格	会员价
PL07732-5mg	5mg	¥5625.00	请登录
PL07732-10mg	10mg	¥8840.00	请登录
PL07732-50mg	50mg	¥26520.00	请登录
PL07732-100mg	100mg	¥36163.00	请登录

Medlife所售产品仅用于科学研究（非临床研究），非药品不可食用，不可用于人体或动物的临床诊断和治疗，我们不为个人提供产品及服务。产品COA等资料，可至下方“质量控制”中下载。

加入购物车在线咨询收藏产品大包装询价

中文名称	Vofopitant
英文名称	Vofopitant
英文别名	3-Piperidinamine,N-[[2-methoxy-5-[5-(trifluoromethyl)-1H-tetrazol-1-yl]phenyl]methyl]-2-phenyl-,(2S,3S)-;VOFOPITANT;(2S-cis)-N-[[2-methoxy-5-[5-(trifluoromethyl)-1H-tetrazol-1yl]phenyl]methyl]-2-phenyl-3-piperidinamine;(3S)-(2-methoxy-5-(5-trifluoromethyltetrazol-1-;[2-methoxy-5-(5-trifluoromethyltetrazol-1-yl)benzyl]-(2S-phenylpiperidin-3S-yl)-amine;[3H]-Vofopitant;3(S)-(2-methoxy-5-(5-trifluoromethyltetrazol-1-yl)phenylmethylamino)-2-(S)-phenylpiperidine;AC1L3TUS;GR 205171;GR 226206;SureCN2996010;UNII-K08BK043YS;Vofopitant [INN];Vofopitant (GR 205171);3-Piperidinamine, N-[[2-methoxy-5-[5-(trifluormethyl)-1H-tetrazol-1-yl]phenyl]methyl]-2-phenyl, (2S,3S);3-Piperidinamine, N-[[2-methoxy-5-[5-(trifluormethyl)-1H-tetrazol-1-yl]phenyl]methyl]-2-phenyl, (2S-cis-)
Cas No.	168266-90-8
分子式	C₂₁H₂₃N₆OF₃
分子量	432.44
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Vofopitant 是一种有效的 NK₁ receptor 拮抗剂，对人，大鼠和雪貂的 NK₁ receptor 的 pK_i 值分别为 10.6，9.5 和 9.8。

生物活性

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.

性状

Solid

IC50 & Target[1][2]

pKi: 10.6 (Human NK1 receptor), 9.5 (Rat NK1 receptor), 9.8 (Ferret NK1 receptor)

体外研究(In Vitro)

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 Ca 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 (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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. 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. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[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.

搜索质检报告(COA)

产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

相关产品

The molarity calculator equation

The dilution calculator equation