|4'-甲氧基-N,N-二甲基-3'-(N-(3-((2-(3-甲基苯甲酰氨基)乙基)氨基)苯基)氨磺酰基)- [1,1'-联苯]-3-甲酰胺|CsnPharm

CAS No.: 1796565-52-0

Orexin 2 Receptor Agonist Catalog No. CSN18036

Synonyms: OX2R;MDK-5220;MDK5220. Orexin2 receptor agonist

Orexin 2 receptor agonist is a potent and selective OX2R agonist with EC50 of 23 nM.

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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Orexins A and B are a pair of neuropeptides that act on two G protein-coupled receptors, orexin receptor-1 (OX1R) and -2 (OX2R), to regulate sleep and wakefulness. Orexin 2 receptor agonist potently activates OX2R with an EC₅₀ value of 23 nM compared to OX1R (EC₅₀ of 1.616 μM). The E_max of orexin 2 receptor agonist against OX2R was 98%. In CHO cells overexpressing hOX1R and HEK-293 cells overexpressing hOX2R, orexin 2 receptor agonist bound to hOX2R and hOX1R with K_i values of 0.14 μM and 0.77 μM, respectively^[2]. In orexin receptor-expressing CHO cells, treatment of orexin 2 receptor agonist led to a robust Ca²⁺ response with 17.6-fold higher potency for OX2R than for OX1R. The response to orexin 2 receptor agonist was fully inhibited by 1 μM of G_q/11 inhibitor UBO-QIC. Orexin 2 receptor agonist also stimulated adenylyl cyclase activity in CHO cells treated with pertussis toxin and GF1092203X^[3].
作用机制The binding of orexin 2 receptor agonist to OX2R induces the inward movements of transmembrane helix 5 and 6, allowing the activity of orexin 2 receptor agonist against OX2R^[2].
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
NCT00608985	-	-	Completed	-	-
NCT02948660	Consciousness Disorders	Phase 4	Recruiting	-	China, Shaanxi ... more >> Department of Neurology, Xijing Hospital, Fourth Military Medical University Recruiting Xi'an, Shaanxi, China, 710032 Contact: Xiai Yang, Master +86 029 84771319 yxa2004.7@163.com Collapse <<
NCT03657355	Healthy Recreational Drug User... more >>s Collapse <<	Phase 1	Recruiting	February 1, 2019	United States, Kansas ... more >> Vince and Associates Clinical Research, Inc. Recruiting Overland Park, Kansas, United States, 66212 Collapse <<

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参考文献

[1] Nagahara T, Saitoh T, et al. Design and Synthesis of Non-Peptide, Selective Orexin Receptor 2 Agonists. J Med Chem. 2015 Oct 22;58(20):7931-7.
[2] Nagahara T, Saitoh T, Kutsumura N, Irukayama-Tomobe Y, Ogawa Y, Kuroda D, Gouda H, Kumagai H, Fujii H, Yanagisawa M, Nagase H. Design and Synthesis of Non-Peptide, Selective Orexin Receptor 2 Agonists. J Med Chem. 2015 Oct 22;58(20):7931-7.
[3] Rinne MK, Leino TO, Turku A, Turunen PM, Steynen Y, Xhaard H, Wallén EAA, Kukkonen JP. Pharmacological characterization of the orexin/hypocretin receptor agonist Nag 26. Eur J Pharmacol. 2018 Oct 15;837:137-144.

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
- 1.7044 mL
- 8.5222 mL
- 17.0445 mL
- 5 mM
- 0.3409 mL
- 1.7044 mL
- 3.4089 mL
- 10 mM
- 0.1704 mL
- 0.8522 mL
- 1.7044 mL

技术信息

CAS号

1796565-52-0

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C32H34N4O5S

运输

蓝冰

分子量

586.70

别名

OX2R;MDK-5220;MDK5220. Orexin2 receptor agonist

溶解度

DMSO	25.0 mg/mL (42.6 mM)

动物实验配方

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NCT00608985	-	-	Completed	-	-
NCT02948660	Consciousness Disorders	Phase 4	Recruiting	-	China, Shaanxi ... more >> Department of Neurology, Xijing Hospital, Fourth Military Medical University Recruiting Xi'an, Shaanxi, China, 710032 Contact: Xiai Yang, Master +86 029 84771319 yxa2004.7@163.com Collapse <<
NCT03657355	Healthy Recreational Drug User... more >>s Collapse <<	Phase 1	Recruiting	February 1, 2019	United States, Kansas ... more >> Vince and Associates Clinical Research, Inc. Recruiting Overland Park, Kansas, United States, 66212 Collapse <<
NCT01243060	Healthy Volunteers	Not Applicable	Completed	-	United States, California ... more >> San Francisco Veterans Affairs Medical Center San Francisco, California, United States, 94121 Collapse <<
NCT03158025	Insomnia Disorders	Phase 1	Completed	-	Canada ... more >> INC Research Toronto, Inc. Toronto, Canada, M5V 2T3 Collapse <<
NCT03755310	Restless Legs Syndrome	Phase 2	Not yet recruiting	March 2020	Spain ... more >> Sleep Research Institute; Paseo de la Habana 151 Not yet recruiting Madrid, Spain, 28036 Contact: Diego García-Berreguero Collapse <<
NCT03025295	Anesthesia	Not Applicable	Recruiting	October 2017	China, Ningxia ... more >> Anesthesiology department of General Hospital of Ningxia Medical University Recruiting Yinchuan, Ningxia, China, 750004 Contact: Zhihua Wang, M.D. Collapse <<
NCT00608985	Primary Insomnia	Phase 3	Completed	-	-

Orexin 2 Receptor Agonist Catalog No. CSN18036

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