MK-3697

Names

[ Name ]:
MK-3697

[Synonym ]:
N-[(5,6-Dimethoxy-2-pyridinyl)methyl]-5'-methyl-5-(1,3-thiazol-2-yl)-2,3'-bipyridine-4-carboxamide
[2,3'-Bipyridine]-4-carboxamide, N-[(5,6-dimethoxy-2-pyridinyl)methyl]-5'-methyl-5-(2-thiazolyl)-
mk-3697

Biological Activity

[Description]:

MK-3697 is an isonicotinamide small molecule, acting as a potent and selective Orexin 2 receptor antagonist with Ki = 0.95 nM.IC50 value: 0.95 nM(Ki)Target: Orexin 2 receptor antagonistMK-3697 is a highly potent, orally bioavailable selective orexin 2 receptor antagonists (2-SORAs) that possess acceptable profiles for clinical development. Herein we report additional SAR studies within the “triaryl” amide 2-SORA series focused on improvements in compound stability in acidic media and time-dependent inhibition of CYP3A4. MK-3697 has improved stability and TDI profiles as well as excellent sleep efficacy across species.

[Related Catalog]:

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

Research Areas >> Neurological Disease

[References]

[1]. Anthony J. Roecker, et al. Discovery of MK-3697: A Selective Orexin 2 Receptor Antagonist (2-SORA) for the Treatment of Insomnia. Bioorganic & Medicinal Chemistry Letters Available online 26 August 2014

[Related Small Molecules]

SB 334867 | lemborexant | Almorexant HCI | Filorexant | Orexin 2 Receptor Agonist | TCS-OX2-29 | MK-1064 | SB-674042 | GSK1059865 | IPSU | SB408124 | Nemorexant | Orexin B (mouse, rat) | SB-649868 | TCS 1102

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Molecular Formula ]:
C₂₃H₂₁N₅O₃S

[ Molecular Weight ]:
447.509

[ Exact Mass ]:
447.136505

[ PSA ]:
127.36000

[ LogP ]:
2.87

[ Index of Refraction ]:
1.622

[ Storage condition ]:
2-8℃

Related Compounds

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