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• 产品描述： SB742457 (GSK 742457)是一种高选择性5-HT6受体拮抗剂，pKi为9.63，比作用于其他受体选择性高100倍以上。Phase 2

• 靶点： 5-HT6:9.63(pKi);5-HTReceptor

• 体外研究：
  Intepirdine (SB742457), a 5-HT6 receptor antagonist, which extends into Alzheimer disease (AD) sufferers further highlights the therapeutic promise of this mechanistic approach. Alzheimer's disease is a devastating neurological condition characterized by a progressive decline in cognitive performance accompanied by behavioral and psychological syndromes, such as depression and psychosis. With the subsequent development of selective 5-HT6 receptor antagonists, preclinical studies in rodents and primates have elucidated the function of this receptor subtype in more detail. It is increasingly clear that blockade of 5-HT6 receptors leads to an improvement of cognitive performance in a wide variety of learning and memory paradigms and also results in anxiolytic and antidepressant-like activity. Intepirdine (SB742457) is generally safe and well tolerated and may be efficacious in Alzheimer disease.

• 体内研究：
  SB-742457是一种有效的，选择性5-HT6受体拮抗剂，在新物体识别测试中，可逆转Scopolamine诱导的学习缺陷，在老年大鼠水迷宫任务中，可提高学习性能

• 参考文献：
  1. Chuang ATT, et al. Alzheimers Dement, 2006, 2, S631–S632 (abstract). 2. Upton N, et al. Neurotherapeutics, 2008, 5(3), 458-469.

• 溶解性： Soluble  in  DMSO、Ethanol

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.829 ml	14.147 ml	28.293 ml
  5 mM	0.566 ml	2.829 ml	5.659 ml
  10 mM	0.283 ml	1.415 ml	2.829 ml
  50 mM	0.057 ml	0.283 ml	0.566 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *