MK-3697 |
Catalog No.GC19250 |
MK-3697은 이소니코틴아미드 소분자로 Ki = 0.95nM인 강력하고 선택적인 Orexin 2 수용체 길항제로 작용합니다.
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Cas No.: 1224846-01-8
Sample solution is provided at 25 µL, 10mM.
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.
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
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