Name: SB742457
Brand: Selleck Chemicals
SKU: S2894
Rating: 5 (2 reviews)

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

CAS: 607742-69-8

Selleck's SB742457 has been cited by 2 Publications

1 Customer Review

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

Related Targets	5-HT1 5-HT2 5-HT3 5-HT4 5-HT6 5-HT7 5-HT5	Click to Expand
Related Compound Libraries	FDA-approved Drug Library Natural Product Library Neuronal Signaling Compound Library CNS-Penetrant Compound Library Anti-alzheimer Disease Compound Library	Click to Expand

Signaling Pathway

5-HT Receptor Signaling Pathway

Choose Selective 5-HT Receptor Inhibitors

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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT00708552	Completed	Alzheimer''s Disease	GlaxoSmithKline	July 4 2008	Phase 2
NCT00551772	Completed	Alzheimer''s Disease	GlaxoSmithKline	August 2007	Phase 1

References

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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

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.
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
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

Tel: +1-832-582-8158 Ext:3
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