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MK-3697
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MK-3697图片
CAS NO:1224846-01-8
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
50mg电议

产品介绍
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 SMILESO=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 tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation 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