SB742457

Catalog No.S2894 Synonyms: GSK 742457

SB742457 Chemical Structure

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.

Size Price Stock Quantity  
In DMSO USD 210 In stock
USD 147 In stock
USD 470 In stock
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Biological Activity

Description SB742457 is a highly selective 5-HT6 receptor antagonist with pKi of 9.63, exhibits >100-fold selectivity over other receptors. Phase 2.
Targets
5-HT6 [1]
9.63(pKi)
In vitro

SB-742457 is a selective 5-HT6 receptor antagonist with cognition, memory, and learning-enhancing effects. [2] 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. [1]

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. [1]

Protocol

Solubility (25°C)

In vitro DMSO 78 mg/mL (220.68 mM)
Ethanol 2 mg/mL (5.65 mM)
Water Insoluble
In vivo Add solvents individually and in order:
2% DMSO, 48% PEG300, 2% Tween 80 and 48% water
5

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 353.44
Formula

C19H19N3O2S

CAS No. 607742-69-8
Storage powder
Synonyms GSK 742457

Bio Calculators

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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

Tech Support

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.

Handling Instructions

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5-HT Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID