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MK-1064

Names

[ CAS No. ]:
1207253-08-4

[ Name ]:
MK-1064

[Synonym ]:
[2,2':5',3''-Terpyridine]-3'-carboxamide, 5''-chloro-N-[(5,6-dimethoxy-2-pyridinyl)methyl]-
5''-Chloro-N-[(5,6-dimethoxy-2-pyridinyl)methyl]-2,2':5',3''-terpyridine-3'-carboxamide
MFCD28502027
MK-1064

Biological Activity

[Description]:

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]

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Orexin Receptor (OX Receptor)
Research Areas >> Cancer

[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.


[Related Small Molecules]

SB 334867 | lemborexant | Almorexant HCI | Filorexant | Orexin 2 Receptor Agonist | TCS-OX2-29 | SB-674042 | GSK1059865 | IPSU | SB408124 | MK-3697 | Nemorexant | Orexin B (mouse, rat) | SB-649868 | TCS 1102

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
662.4±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C24H20ClN5O3

[ Molecular Weight ]:
461.900

[ Flash Point ]:
354.4±31.5 °C

[ Exact Mass ]:
461.125458

[ LogP ]:
3.04

[ Vapour Pressure ]:
0.0±2.0 mmHg at 25°C

[ Index of Refraction ]:
1.619

[ Storage condition ]:
2-8℃

Related Compounds