Catalog No.S2894

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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SB742457 Chemical Structure

SB742457 Chemical Structure
Molecular Weight: 353.44

Validation & Quality Control

Quality Control & MSDS

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SB742457 is available in the following compound libraries:

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Product Description

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]
IC50 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(Only for Reference)

Animal Study: [1]

Animal Models Aged rats with spatial task deficits
Dosages 1.5 mg/kg
Administration Orally

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Chuang ATT, et al. Alzheimers Dement, 2006, 2, S631–S632 (abstract).

[2] Upton N, et al. Neurotherapeutics, 2008, 5(3), 458-469.

Clinical Trial Information( data from, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
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

Chemical Information

Download SB742457 SDF
Molecular Weight (MW) 353.44


CAS No. 607742-69-8
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms GSK 742457
Solubility (25°C) * In vitro DMSO 78 mg/mL (220.68 mM)
Ethanol 2 mg/mL (5.65 mM)
Water <1 mg/mL
In vivo 2% DMSO, 48% PEG300, 2% Tween 80 and 48% water 5
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name Quinoline, 3-(phenylsulfonyl)-8-(1-piperazinyl)-

Tech Support

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