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MK-1064

Cat. No. M8997

All AbMole products are for research use only, cannot be used for human consumption.

MK-1064 Structure
Size Price Availability Quantity
5mg USD 205  USD205 In stock
10mg USD 330  USD330 In stock
25mg USD 670  USD670 In stock
50mg USD 960  USD960 In stock
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Quality Control & Documentation
Biological Activity

MK-1064 is a potent, selective and orally active Orexin OX2 Receptor Antagonist for the research of insomnia. 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.

Chemical Information
Molecular Weight 461.9
Formula C24H20ClN5O3
CAS Number 1207253-08-4
Solubility (25°C) DMSO 10 mM
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Leslie R Amodeo, et al. Alcohol Clin Exp Res. Effects of an Orexin-2 Receptor Antagonist on Sleep and Event-Related Oscillations in Female Rats Exposed to Chronic Intermittent Ethanol During Adolescence

[2] Kanta Kon, et al. J Endocrinol. Chronotherapeutic effect of orexin antagonists on glucose metabolism in diabetic mice

[3] Gao M, et al. Bioorg Med Chem Lett. Synthesis of [(11)C]MK-1064 as a new PET radioligand for imaging of orexin-2 receptor.

[4] Gotter AL, et al. Sci Rep. Orexin 2 Receptor Antagonism is Sufficient to Promote NREM and REM Sleep from Mouse to Man.

[5] Anthony J Roecker, et al. ChemMedChem. 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

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Keywords: MK-1064 supplier, OX Receptor, inhibitors, activators

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