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Intepirdine

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Chemical Structure| 607742-69-8 同义名 : SB-742457;GSK-742457;RVT101. intepirdine.;RVT-101
CAS号 : 607742-69-8
货号 : A879799
分子式 : C19H19N3O2S
纯度 : 99%+
分子量 : 353.438
MDL号 : MFCD12828872
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(141.47 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：

2% DMSO+48% PEG300+2% Tween 80 +48% water 5 mg/mL

生物活性
靶点

  • 5-HT6

    5-HT6, pKi:9.63
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.83mL

0.57mL

0.28mL

14.15mL

2.83mL

1.41mL

28.29mL

5.66mL

2.83mL
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.