MK-1064

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Chemical Information

Product name：MK-1064	Purity：99% min
CAS NO：1207253-08-4	Solubility：DMSO : 50 mg/mL (108.25 mM)
Molecular Formula：C₂₄H₂₀ClN₅O₃	Package：Packaging according to customer requirements
Molecular Weight：461.900	Storage：Store at -20℃

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Remarks

MK-1064 is a potent, selective and orally active Orexin OX2 Receptor Antagonist for potential treatment of insomnia. Preclinically, 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. Similar to dual antagonists, MK-1064 increases NREM and REM sleep in dogs without inducing cataplexy.

References

[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.