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MK 6096
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MK 6096图片
CAS NO:1088991-73-4
规格:98%
分子量:420.48
包装与价格:
包装价格(元)
5mg电议
25mg电议
100mg电议

产品介绍
OX1/OX2 receptor antagonist
CAS:1088991-73-4
分子式:C24H25FN4O2
分子量:420.48
纯度:98%
存储:Store at -20°C

Background:

Filorexant (MK-6096) is an orally bioavailable potent and selective reversible antagonist of OX1 and OX2 receptor(<3 nM in binding).


In radioligand binding and functional cell based assays Filorexant (MK-6096) demonstrated potent binding and antagonism of both human OX(1)R and OX(2)R (170 receptors and enzymes. Filorexant (MK-6096) occupies 90% of human OX(2)Rs expressed in transgenic rats at a plasma concentration of 142 nM.


Filorexant (MK-6096) dose-dependently reduced locomotor activity and significantly increased sleep in rats (3-30 mg/kg) and dogs (0.25 and 0.5 mg/kg).


参考文献:
[1]. Winrow CJ, et al. Pharmacological characterization of MK-6096 - a dual orexin receptor antagonist for insomnia. Neuropharmacology. 2012 Feb;62(2):978-87.
[2]. Coleman PJ, et al. Discovery of [(2R,5R)-5-{[(5-fluoropyridin-2-yl)oxy]methyl}-2-methylpiperidin-1-yl][5-methyl-2-(pyrimidin-2-yl)phenyl]methanone (MK-6096): a dual orexin receptor antagonist with potent sleep-promoting properties. ChemMedChem. 2012 Mar 5;7(3):415-24, 337.