MK-1064

An orexin 2 receptor antagonist

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1mg

￥912.00

730.00

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5mg

￥1725.00

1380.00

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10mg

￥2725.00

2180.00

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25mg

￥5400.00

4320.00

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50mg

￥7850.00

6280.00

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货号: ajci22740
CAS: 1207253-08-4
别名:
分子式: C24H20ClN5O3
分子量: 461.9
纯度: >98%
溶解度: DMSO : 50 mg/mL (108.25 mM);Water : < 0.1 mg/mL (insoluble)
储存: Store at -20°C
库存: 现货

Background

MK-1064 is a selective orexin 2 receptor antagonist (2-SORA) for the research of insomnia.target: 2-SORA [1]In vivo: MK-1064 promotes sleep and increases both rapid eye movement (REM) and non-REM (NREM) sleep in rats at OX2R occupancies higher than the range observed for dual orexin receptor antagonists. MK-1064 increases NREM and REM sleep in dogs without inducing cataplexy. The reference for animal administration is 30 mg/kg. [2]

参考文献:
[1]. Roecker AJ et al. Discovery of 5''-chloro-N-[(5,6-dimethoxypyridin-2-yl)methyl]-2,2':5',3''-terpyridine-3'-carboxamide (MK-1064): a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia. ChemMedChem. 2014 Feb;9(2):311-22.
[2]. Gotter AL et al. Orexin 2 Receptor Antagonism is Sufficient to Promote NREM and REM Sleep from Mouse to Man. Sci Rep. 2016 Jun 3;6:27147.