|5''-氯-N-((5,6-二甲氧基吡啶-2-基)甲基)-[2,2':5',3''-三联吡啶]-3'-甲酰胺|CsnPharm

CAS No.: 1207253-08-4

MK-1064 Catalog No. CSN18852

Synonyms: MK 1064

MK-1064 is a selective orexin 2 receptor antagonist(2-SORA) for the research of insomnia.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述MK-1064 is a potent and selective orexin2 receptor antagonist with Ki value of 0.5nM (determined using a radio ligand-displacement binding assay) and IC50 value of 18nM (determined by FLIPR assay). Oral administration of MK-1064 promoted sleep of mice at dose of 100mg/kg and of rat at dose of 30mg/kg. Pretreatment with MK-1064 (30mg/kg, p.o.) reduced adrenocorticotropic hormone levels of restrained rats with further stimulated orexins by DREADDs on day 5.
动物研究
剂量
Mice: 30 mg/kg^[3] (p.o.), 10 mg/kg - 100 mg/kg^[4] (p.o.) Rat: 0.3 mg/kg - 20 mg/kg^[3] (p.o.)

给药途径
p.o.
临床研究
NCT号适应症或疾病临床期招募状态预计完成时间地点
NCT02549027 Polysomnography Phase 1 Completed - -
NCT02549027 - - Completed - -
NCT02549014 Pharmacokinetics Phase 1 Completed - -
更多
参考文献

动物研究
剂量	Mice: 30 mg/kg^[3] (p.o.), 10 mg/kg - 100 mg/kg^[4] (p.o.) Rat: 0.3 mg/kg - 20 mg/kg^[3] (p.o.)
给药途径	p.o.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02549027	Polysomnography	Phase 1	Completed	-	-
NCT02549027	-	-	Completed	-	-
NCT02549014	Pharmacokinetics	Phase 1	Completed	-	-

[1] Staton CD, Yaeger JDW, et al. Orexin 2 receptor stimulation enhances resilience, while orexin 2 inhibition promotes susceptibility, to social stress, anxiety and depression. Neuropharmacology. 2018 Dec;143:79-94.
[2] Grafe LA, Eacret D, 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.
[3] Gotter AL, Forman MS, 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.
[4] Delineating the influence of orexin 1 and 2 receptors on sleep architecture and aversive memory

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1650 mL
- 10.8248 mL
- 21.6497 mL
- 5 mM
- 0.4330 mL
- 2.1650 mL
- 4.3299 mL
- 10 mM
- 0.2165 mL
- 1.0825 mL
- 2.1650 mL

技术信息

CAS号

1207253-08-4

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H20ClN5O3

运输

蓝冰

分子量

461.90

别名

MK 1064

溶解度

DMSO	92.0 mg/mL (199.2 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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