Catalog No.S2894 Synonyms: GSK 742457
Molecular Weight(MW): 353.44
SB742457 is a highly selective 5-HT6 receptor antagonist with pKi of 9.63, exhibits >100-fold selectivity over other receptors. Phase 2.
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Choose Selective 5-HT Receptor Inhibitors
|Description||SB742457 is a highly selective 5-HT6 receptor antagonist with pKi of 9.63, exhibits >100-fold selectivity over other receptors. Phase 2.|
SB-742457 is a selective 5-HT6 receptor antagonist with cognition, memory, and learning-enhancing effects.  SB-742457 is a novel cognitive enhancing agent for Alzheimer's disease. SB-742457 is a potential agent added to stablize donepezil treatment in subjects with mild-to-moderate Alzheimer's disease. 
|In vivo||SB-742457 is a potent and selective 5-HT6 receptor antagonist that is shown to reverse a scopolamine induced learning deficit in the novel object recognition test and to enhance performance in a water maze task by aged rats. |
|In vitro||DMSO||78 mg/mL (220.68 mM)|
|Ethanol||2 mg/mL (5.65 mM)|
|In vivo||2% DMSO, 48% PEG300, 2% Tween 80 and 48% water||5|
* 1 mg/ml means slightly soluble or insoluble.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT00710684||Completed||Mild-to-moderate Alzheimers Disease|Alzheimers Disease||GlaxoSmithKline||July 2008||Phase 2|
|NCT00708552||Completed||Alzheimers Disease||GlaxoSmithKline||July 2008||Phase 2|
|NCT00551772||Completed||Alzheimers Disease||GlaxoSmithKline||August 2007||Phase 1|
|NCT00348192||Completed||Alzheimers Disease||GlaxoSmithKline||May 2006||Phase 2|
|NCT00224497||Completed||Alzheimers Disease||GlaxoSmithKline||September 2005||Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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