Home Neuronal Signaling 5-HT Receptor antagonist SB742457

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SB742457 5-HT Receptor antagonist

Cat.No.S2894

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 5-HT Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 353.44

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 353.44 Formula

C19H19N3O2S

 Storage (From the date of receipt)
CAS No. 607742-69-8 Download SDF Storage of Stock Solutions

Synonyms GSK 742457 Smiles C1CN(CCN1)C2=CC=CC3=CC(=CN=C32)S(=O)(=O)C4=CC=CC=C4

Solubility

In vitro
Batch:

DMSO : 78 mg/mL (220.68 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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.
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Mechanism of Action

Targets/IC50/Ki
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]
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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