Home Neuronal Signaling 5-HT Receptor antagonist SB742457 For research use only.

SB742457

Synonyms: GSK 742457

SB742457 (GSK 742457) is a highly selective 5-HT6 receptor antagonist with pKi of 9.63, exhibits >100-fold selectivity over other receptors. Phase 2.

SB742457 Chemical Structure

SB742457 Chemical Structure

CAS No. 607742-69-8

Purity & Quality Control

Batch: S289401 DMSO]78 mg/mL]false]Ethanol]2 mg/mL]false]Water]Insoluble]false Purity: 99.51%
99.51

SB742457 Related Products

Signaling Pathway

5-HT Receptor Signaling Pathways

5-HT Receptor Signaling Pathway

Biological Activity

Description SB742457 (GSK 742457) 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
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00708552 Completed
Alzheimer''s Disease
GlaxoSmithKline
 July 4 2008 Phase 2
NCT00551772 Completed
Alzheimer''s Disease
GlaxoSmithKline
 August 2007 Phase 1

Chemical Information & Solubility

Molecular Weight 353.44 Formula

C19H19N3O2S
CAS No. 607742-69-8 SDF Download SB742457 SDF
Smiles C1CN(CCN1)C2=CC=CC3=CC(=CN=C32)S(=O)(=O)C4=CC=CC=C4
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 78 mg/mL ( (220.68 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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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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