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SB742457
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SB742457图片
CAS NO:607742-69-8
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
25mg电议

产品介绍
SB742457 (SB742457) 是一种高选择性 5-HT6 受体拮抗剂,pKi 为 9.63;表现出比其他受体高 100 倍的选择性。
Cas No.607742-69-8
别名3-苯基磺酰基-8-(哌嗪-1-基)喹啉,SB-742457; GSK-742457; RVT-101
化学名3-(benzenesulfonyl)-8-piperazin-1-ylquinoline
Canonical SMILESC1CN(CCN1)C2=CC=CC3=CC(=CN=C32)S(=O)(=O)C4=CC=CC=C4
分子式C19H19N3O2S
分子量353.44
溶解度≥ 17.65mg/mL in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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