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MK-1064
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-1064图片
CAS NO:1207253-08-4
包装与价格：
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
MK-1064 是一种选择性和口服活性的 OX2R 拮抗剂（Ki:0.5 nM，IC50:18 nM）。
Cas No.1207253-08-4
Canonical SMILESO=C(C1=CC(C2=CC(Cl)=CN=C2)=CN=C1C3=NC=CC=C3)NCC4=NC(OC)=C(OC)C=C4
分子式C24H20ClN5O3
分子量461.9
溶解度DMSO : 50 mg/mL (108.25 mM);Water :< 0.1 mg/mL (insoluble)
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-1064 is a selective orexin 2 receptor antagonist (2-SORA) for the research of insomnia.target: 2-SORA [1]In vivo: MK-1064 promotes sleep and increases both rapid eye movement (REM) and non-REM (NREM) sleep in rats at OX2R occupancies higher than the range observed for dual orexin receptor antagonists. MK-1064 increases NREM and REM sleep in dogs without inducing cataplexy. The reference for animal administration is 30 mg/kg. [2]

References:
[1]. Roecker AJ et al. Discovery of 5''-chloro-N-[(5,6-dimethoxypyridin-2-yl)methyl]-2,2':5',3''-terpyridine-3'-carboxamide (MK-1064): a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia. ChemMedChem. 2014 Feb;9(2):311-22.
[2]. Gotter AL et al. Orexin 2 Receptor Antagonism is Sufficient to Promote NREM and REM Sleep from Mouse to Man. Sci Rep. 2016 Jun 3;6:27147.