| Bioactivity | 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 | MK-3697 | ||||||||||||
| CAS | 1224846-01-8 | ||||||||||||
| Formula | C23H21N5O3S | ||||||||||||
| Molar Mass | 447.51 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [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 |
MK-3697
CAS: 1224846-01-8 F: C23H21N5O3S W: 447.51
MK-3697 is an isonicotinamide small molecule, acting as a potent and selective Orexin 2 receptor antagonist with Ki = 0.
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