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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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
|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|
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