产品说明书

MK-1064

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Chemical Structure| 1207253-08-4 同义名 : -
CAS号 : 1207253-08-4
货号 : A827816
分子式 : C24H20ClN5O3
纯度 : 97%
分子量 : 461.9
MDL号 : MFCD28502027
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(108.25 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 MK-1064 serves as a specific, orally effective OX2R antagonist, with a Ki of 0.5 nM and an IC50 of 18 nM, and is observed to facilitate sleep in live models, suggesting its potential for insomnia research[1].[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.16mL

0.43mL

0.22mL

10.82mL

2.16mL

1.08mL

21.65mL

4.33mL

2.16mL
参考文献

[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.

[3]Laura A Grafe, et al. Orexin 2 receptor regulation of the hypothalamic-pituitary-adrenal (HPA) response to acute and repeated stress. Neuroscience. 2017 Apr 21;348:313-323.