380899-24-1|SB-649868|CsnPharm

CAS No.: 380899-24-1

SB-649868 Catalog No. CSN20633

Synonyms: GSK649868

SB-649868 is a potent and selective orally active orexin (OX) 1 and OX2 receptor antagonist (pKi =9.4 and 9.5 at the OX1 and OX2 receptor, respectively).

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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The orexin-1 (OX₁) and orexin-2 (OX₂) receptors are G-protein coupled receptors profoundly implicated in sleep disorders. SB-649868 is a dual OX₁ and OX₂ receptor antagonist with pK_i values of 9.4 and 9.5 for human OX₁ and OX₂ receptors, respectively. It demonstrates higher functional potencies for rat OX₁ and OX₂ receptors with pK_i values of 9.93 and 10.11, respectively. The in vitro clearance of SB-649868 in rat and human liver microsomes was 8.7 and 15.1mL/min/g, respectively. SB-649868 displaced [³H]almorexant in Chinese hamster ovary cells overexpressing both human recombinant OX₁ and OX₂ receptors in a concentration dependent manner, with pK_i values of 9.12 and 8.89, respectively, In rats subjected to intracerebroventricular injection of neuropeptides orexin-A (OX-A), oral administration of SB-649868 (3 and 10mg/kg) 3 hours before OX-A injection resulted in a significant, dose-dependent reduction of OX-A induced grooming. In the circadian time model of male CD rats, SB-649868 treatment caused a dose-dependent reduction in sleep latency, with the maximal effect observed at 30mg/kg. SB-649868 at 10 and 30mg/kg also significantly increased total sleep time over the 5-hour testing period in a dose-dependent manner^[3].
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
NCT00440323	Sleep Initiation and Maintenan... more >>ce Disorders Collapse <<	Phase 1	Completed	-	United Kingdom ... more >> GSK Investigational Site Guildford, Surrey, United Kingdom, GU2 7XP Collapse <<
NCT00495274	Sleep Initiation and Maintenan... more >>ce Disorders Collapse <<	Phase 1	Completed	-	Italy ... more >> GSK Investigational Site Verona, Veneto, Italy, 37134 Collapse <<
NCT00495729	Sleep Initiation and Maintenan... more >>ce Disorders Collapse <<	Phase 1	Completed	-	Germany ... more >> GSK Investigational Site Berlin, Germany, 14050 Collapse <<

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参考文献

[1] Faedo S, Perdona E, et al. Functional and binding kinetic studies make a distinction between OX1 and OX2 orexin receptor antagonists. Eur J Pharmacol. 2012 Oct 5;692(1-3):1-9.
[2] Di Fabio R, Pellacani A, et al. Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5562-7.
[3] Di Fabio R, Pellacani A, Faedo S, Roth A, Piccoli L, Gerrard P, Porter RA, Johnson CN, Thewlis K, Donati D, Stasi L, Spada S, Stemp G, Nash D, Branch C, Kindon L, Massagrande M, Poffe A, Braggio S, Chiarparin E, Marchioro C, Ratti E, Corsi M. Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5562-7.

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
- 2.0940 mL
- 10.4701 mL
- 20.9402 mL
- 5 mM
- 0.4188 mL
- 2.0940 mL
- 4.1880 mL
- 10 mM
- 0.2094 mL
- 1.0470 mL
- 2.0940 mL

技术信息

CAS号

380899-24-1

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H24FN3O3S

运输

蓝冰

分子量

477.55

别名

GSK649868

溶解度

DMSO	95.0 mg/mL (198.9 mM) warming

动物实验配方

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT00440323	Sleep Initiation and Maintenan... more >>ce Disorders Collapse <<	Phase 1	Completed	-	United Kingdom ... more >> GSK Investigational Site Guildford, Surrey, United Kingdom, GU2 7XP Collapse <<
NCT00495274	Sleep Initiation and Maintenan... more >>ce Disorders Collapse <<	Phase 1	Completed	-	Italy ... more >> GSK Investigational Site Verona, Veneto, Italy, 37134 Collapse <<
NCT00495729	Sleep Initiation and Maintenan... more >>ce Disorders Collapse <<	Phase 1	Completed	-	Germany ... more >> GSK Investigational Site Berlin, Germany, 14050 Collapse <<
NCT01299597	Sleep Disorders	Phase 1	Completed	-	Germany ... more >> GSK Investigational Site Berlin, Germany, 14050 Collapse <<
NCT00426816	Sleep Initiation and Maintenan... more >>ce Disorders Collapse <<	Phase 2	Completed	-	Germany ... more >> GSK Investigational Site Mannheim, Baden-Wuerttemberg, Germany, 68159 GSK Investigational Site Cottbus, Brandenburg, Germany, 03050 GSK Investigational Site Schwerin, Mecklenburg-Vorpommern, Germany, 19055 GSK Investigational Site Dortmund, Nordrhein-Westfalen, Germany, 44263 GSK Investigational Site Muenster, Nordrhein-Westfalen, Germany, 48149 GSK Investigational Site Dresden, Sachsen, Germany, 01307 GSK Investigational Site Berlin, Germany, 10117 GSK Investigational Site Berlin, Germany, 10787 GSK Investigational Site Berlin, Germany, 13125 GSK Investigational Site Hamburg, Germany, 20249 Collapse <<
NCT00534872	Insomnia	Phase 1	Withdrawn(The study was stoppe... more >>nd before recruitment start for preclinical safety finding in rats.) Collapse <<	October 2007	-
NCT01030939	Sleep Disorders	Phase 1	Completed	-	Germany ... more >> GSK Investigational Site Berlin, Germany, 14050 Collapse <<
NCT00520663	Sleep Initiation and Maintenan... more >>ce Disorders Collapse <<	Phase 1	Completed	-	United Kingdom ... more >> GSK Investigational Site Tranent, West Lothian, United Kingdom, EH33 2NE Collapse <<

SB-649868 Catalog No. CSN20633

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