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首页-小分子抑制剂&激动剂-GPCR-Neurokinin Receptor-Vofopitant
Vofopitant

Chemical Structure : Vofopitant

CAS No.: 168266-90-8

Vofopitant (GR205171)

货号: PC-23397Not For Human Use, Lab Use Only.

Vofopitant (GR205171) is a potent, selective and orally available tachykinin neurokinin 1(NK1) receptor antagonist, inhibits [3H]SP binding to the NK1 receptor with pKi values of 9.5 and 10.6 in rat and human membranes respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

Vofopitant (GR205171) is a potent, selective and orally available tachykinin neurokinin 1(NK1) receptor antagonist, inhibits [3H]SP binding to the NK1 receptor with pKi values of 9.5 and 10.6 in rat and human membranes respectively.
Vofopitant prevents vagal stimulation-induced retching but not neuronal transmission from emetic vagal afferents to solitary nucleus neurons in dogs.
Vofopitant exhibits an acute response to cisplatin but does not vomit during the delayed phase.

物理化学性质&存储条件

分子量 432.45
分子式 C21H23F3N6O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(2S,3S)-N-(2-Methoxy-5-(5-(trifluoromethyl)-1H-tetrazol-1-yl)benzyl)-2-phenylpiperidin-3-amine

参考文献

1. Gardner CJ, et al. Regul Pept. 1996 Aug 27;65(1):45-53.

2. Gobert A, et al. Neuropsychopharmacology. 2009 Mar;34(4):1039-56.

3. Heldt SA, et al. Behav Pharmacol. 2009 Oct;20(7):584-95.

4. Malik NM, et al. Eur J Pharmacol. 2007 Jan 26;555(2-3):164-73.

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