SB742457

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

Related Compound Libraries

SB742457 is available in the following compound libraries:

Product Information

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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]
Features

Protocol(Only for Reference)

Animal Study: [1]

Animal Models Aged rats with spatial task deficits
Formulation
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)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
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

References

[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 http://clinicaltrials.gov, updated on 2016-07-23)

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

Chemical Information

Download SB742457 SDF
Molecular Weight (MW) 353.44
Formula

C19H19N3O2S

CAS No. 607742-69-8
Storage 3 years -20℃powder
6 months-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 (<1 mM)
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

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.

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