1224846-01-8

1224846-01-8 structure

Name: MK-3697
Chemical Name: N-[(5,6-dimethoxypyridin-2-yl)methyl]-5'-methyl-5-(1,3-thiazol-2-yl)-2,3'-bipyridine-4-carboxamide
CAS Number: 1224846-01-8
Molecular Formula: C₂₃H₂₁N₅O₃S
Molecular Weight: 447.509
Catalog: Signaling Pathways GPCR/G Protein Orexin Receptor (OX Receptor)
Create Date: 2017-10-28 02:09:58
Modify Date: 2024-01-12 12:05:58
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.

Name	N-[(5,6-dimethoxypyridin-2-yl)methyl]-5'-methyl-5-(1,3-thiazol-2-yl)-2,3'-bipyridine-4-carboxamide
Synonyms	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

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