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SB742457

现货
Catalog No.
B2256
5-HT6受体拮抗剂,具有高选择性和高亲和力。
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,570.00
现货
5mg
¥ 1,050.00
现货
25mg
¥ 3,300.00
现货

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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
Solubility≥17.65mg/mL in DMSO
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
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

生物活性

描述 SB742457是5-HT6受体的高选择性拮抗剂,pKi值为9.63。
靶点 5-HT6          
IC50 9.63(pKi)          

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