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CAS No.: 607742-69-8

Intepirdine Catalog No. CSN16751

Synonyms: SB-742457;GSK-742457;RVT-101

SB-742457 is a selective 5-HT6 receptor antagonist with Ki value of 1.4 nM, showing potential cognition, memory, and learning-enhancing effects.

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生物活性

实验方案

技术信息

生物活性

描述SB-742457 is a 5-HT6 receptor antagonist with a pKi of 9.63, which is more than 100 times higher than other receptors. In vivo, acute administration of SB742457 (3 mg/kg, po) significantly improved performance of the MA (megaloblasticanemia) rats. Chronic administration of SB742457 (3 mg/kg) reversed the age-related deficit of the MA to match their performance to that of YG rats^[3]. In vitro, the cognitive enhancing properties of SB-742457 extends into AD sufferers further highlights the therapeutic promise of this mechanistic approach^[4].
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
NCT02669433	Dementia With Lewy Bodies	Phase 2	Completed	-	-
NCT02910102	Alzheimer's Disease ... more >> Dementia With Lewy Bodies Parkinson's Disease Dementia Collapse <<	Phase 2	Completed	-	United States, Arizona ... more >> US101 Phoenix, Arizona, United States, 85013 United States, California US118 Simi Valley, California, United States, 93065 US117 Temecula, California, United States, 92591 United States, Florida US115 Boca Raton, Florida, United States, 33431 US109 Hallandale Beach, Florida, United States, 33009 US116 Miami, Florida, United States, 33137 US108 Pensacola, Florida, United States, 32502 United States, Georgia US106 Columbus, Georgia, United States, 31909 United States, Indiana US107 Indianapolis, Indiana, United States, 46202 United States, Michigan US102 Ann Arbor, Michigan, United States, 48106 United States, Ohio US111 Columbus, Ohio, United States, 43210 Collapse <<
NCT02586909	Alzheimer's Disease	Phase 3	Terminated(Intepirdine did not... more >> meet its primary efficacy endpoints in lead-in study RVT-101-3001.) Collapse <<	-	-

更多
参考文献

[1] Callaghan CK, Hok V, et al. Age-related declines in delayed non-match-to-sample performance (DNMS) are reversed by the novel 5HT6 receptor antagonist SB742457. Neuropharmacology. 2012 Oct;63(5):890-7.
[2] Codony X, Vela JM, Ramirez MJ. 5-HT(6) receptor and cognition. Curr Opin Pharmacol. 2011 Feb;11(1):94-100.
[3] Callaghan CK, Hok V, Della-Chiesa A, Virley DJ, Upton N, O'Mara SM. Age-related declines in delayed non-match-to-sample performance (DNMS) are reversed by the novel 5HT6 receptor antagonist SB742457. Neuropharmacology. 2012;63(5):890-897.
[4] Upton N, Chuang TT, Hunter AJ, Virley DJ. 5-HT6 receptor antagonists as novel cognitive enhancing agents for Alzheimer's disease. Neurotherapeutics. 2008;5(3):458-469.

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
- 2.8293 mL
- 14.1467 mL
- 28.2935 mL
- 5 mM
- 0.5659 mL
- 2.8293 mL
- 5.6587 mL
- 10 mM
- 0.2829 mL
- 1.4147 mL
- 2.8293 mL

技术信息

CAS号

607742-69-8

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H19N3O2S

运输

蓝冰

分子量

353.44

别名

SB-742457;GSK-742457;RVT-101;RVT101. intepirdine

溶解度

DMSO	80.0 mg/mL (226.3 mM) warming
Water	insoluble

动物实验配方

2% DMSO+48% PEG300+2% Tween 80 +48% water

5 mg/mL

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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

NCT02669433	Dementia With Lewy Bodies	Phase 2	Completed	-	-
NCT02910102	Alzheimer's Disease ... more >> Dementia With Lewy Bodies Parkinson's Disease Dementia Collapse <<	Phase 2	Completed	-	United States, Arizona ... more >> US101 Phoenix, Arizona, United States, 85013 United States, California US118 Simi Valley, California, United States, 93065 US117 Temecula, California, United States, 92591 United States, Florida US115 Boca Raton, Florida, United States, 33431 US109 Hallandale Beach, Florida, United States, 33009 US116 Miami, Florida, United States, 33137 US108 Pensacola, Florida, United States, 32502 United States, Georgia US106 Columbus, Georgia, United States, 31909 United States, Indiana US107 Indianapolis, Indiana, United States, 46202 United States, Michigan US102 Ann Arbor, Michigan, United States, 48106 United States, Ohio US111 Columbus, Ohio, United States, 43210 Collapse <<
NCT02586909	Alzheimer's Disease	Phase 3	Terminated(Intepirdine did not... more >> meet its primary efficacy endpoints in lead-in study RVT-101-3001.) Collapse <<	-	-
NCT02928445	Dementia With Lewy Bodies	Phase 2 Phase 3	Terminated(Intepirdine did not... more >> meet its primary efficacy endpoints in the lead-in study RVT-101-2001.) Collapse <<	-	-
NCT02585934	Alzheimer's Disease	Phase 3	Completed	-	-
NCT00348192	Alzheimer's Disease	Phase 2	Completed	-	Austria ... more >> GSK Investigational Site Hall in Tirol, Austria, A-6060 GSK Investigational Site Vienna, Austria, A-1130 GSK Investigational Site Vienna, Austria, A-1220 Bulgaria GSK Investigational Site Sofia, Bulgaria, 1113 GSK Investigational Site Sofia, Bulgaria, 1431 GSK Investigational Site Varna, Bulgaria, 9010 Chile GSK Investigational Site Providencia / Santiago, Región Metro De Santiago, Chile, 7500710 GSK Investigational Site Santiago, Región Metro De Santiago, Chile, 7560356 GSK Investigational Site Valparaiso, Valparaíso, Chile, 2352499 Estonia GSK Investigational Site Tallinn, Estonia, 10617 GSK Investigational Site Tartu, Estonia, 51014 Germany GSK Investigational Site Ostfildern, Baden-Wuerttemberg, Germany, 73760 GSK Investigational Site Huettenberg, Hessen, Germany, 35625 GSK Investigational Site Achim, Niedersachsen, Germany, 28832 GSK Investigational Site Baesweiler, Nordrhein-Westfalen, Germany, 52499 GSK Investigational Site Hattingen, Nordrhein-Westfalen, Germany, 45525 Russian Federation GSK Investigational Site Moscow, Russian Federation, 115552 GSK Investigational Site Moscow, Russian Federation, 117049 GSK Investigational Site St. Petersburg, Russian Federation, 197022 GSK Investigational Site St.-Petersburg, Russian Federation, 198103 Slovakia GSK Investigational Site Bratislava, Slovakia, 811 01 GSK Investigational Site Bratislava, Slovakia, 826 06 GSK Investigational Site Bratislava, Slovakia, 831 03 United Kingdom GSK Investigational Site Bradford, United Kingdom, BD7 1HR GSK Investigational Site Swindon, United Kingdom, SN1 4HZ GSK Investigational Site West of Scotland Science Park, Glasgow, United Kingdom, G20 0XA Collapse <<
NCT02585934	-	-	Completed	-	-
NCT00224497	Alzheimer's Disease	Phase 2	Completed	-	-
NCT00708552	Alzheimer's Disease	Phase 2	Completed	-	-
NCT00551772	Alzheimer's Disease	Phase 1	Completed	-	United States, Indiana ... more >> GSK Investigational Site Evansville, Indiana, United States, 47714 Collapse <<
NCT00708552	-	-	Completed	-	-
NCT00710684	Alzheimer's Disease	Phase 2	Completed	-	-
NCT00710684	-	-	Completed	-	-

Intepirdine Catalog No. CSN16751

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