MK-3697 是一种异烟酰胺小分子，是一种有效的选择性 Orexin 2 受体拮抗剂，Ki = 0.95 nM。
| Cas No. | 1224846-01-8 |
| Canonical SMILES | O=C(C1=CC(C2=CC(C)=CN=C2)=NC=C1C3=NC=CS3)NCC4=NC(OC)=C(OC)C=C4 |
| 分子式 | C23H21N5O3S |
| 分子量 | 447.51 |
| 溶解度 | DMSO : 22.5 mg/mL (50.28 mM) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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 |
