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SB742457

Catalog No.
B2256
5-HT6 receptor antagonist,highly selective and high affinity
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$157.00
In stock
5mg
$105.00
In stock
25mg
$330.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

SB742457 is a selective antagonist of 5-HT6 receptor with a pKi value of 9.63 [1].

SB742457 has been found to be a highly selective 5-HT6 receptor antagonist with high affinity to human 5-HT6 receptor. The pKi value of SB742457 is 9.63. In addition, because of the orally bioavailable, SB742457 has been reported to promote brain penetration in rat over previously developed compounds. Besides, subchronic daily oral pre-dosing of SB742457 (1.5mg/kg) has been noted to significantly induce by the cholinergic antagonist scopolamine (0.5mg/kg) in a novel object recognition paradigm. Apart from these, acute oral treatment of SB742457 has been found to induce significant increases levels of glutamate and acetylcholine in extracellular in the medial prefrontal cortex of freely moving rats [1].

Reference:
[1] Aaron T. T. Chuang, Andrew Foley, Perdita L. Pugh, David Sunter, Xin Tong, Ciaran Regan, Lee A. Dawson, Andrew D. Medhurst, Neil Upton.5-HT6 receptor antagonist SB-742457 as a novel cognitive enhancing agent for Alzheimer’s disease. Alzheimer's & Dementia: The Journal of the Alzheimer's Association Volume 2, Issue 3, Supplement, Pages S631–S632, July 2006

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt353.44
Cas No.607742-69-8
FormulaC19H19N3O2S
Solubilityinsoluble in H2O; ≥17.65 mg/mL in DMSO; ≥2.13 mg/mL in EtOH with gentle warming and ultrasonic
Chemical Name3-(benzenesulfonyl)-8-piperazin-1-ylquinoline
SDFDownload SDF
Canonical SMILESC1CN(CCN1)C2=CC=CC3=CC(=CN=C32)S(=O)(=O)C4=CC=CC=C4
Shipping ConditionShip with blue ice, or upon other requests.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon.

Biological Activity

Description SB742457 is a highly selective antagonist of 5-HT6 receptor with a pKi value of 9.63.
Targets 5-HT6          
IC50 9.63(pKi)          

Quality Control

Chemical structure

SB742457