WAY-181187 (Synonyms: SAX-187)
目录号: PL04001 纯度: ≥98%
CAS No. :554403-49-5
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中文名称
WAY-181187
中文别名
2-[1-(6-氯-咪唑并[2,1-b]噻唑-5-磺酰基)-1H-吲哚-3-基]-乙胺;2-[1-[(6-氯咪唑并[2,1-b][1,3]噻唑-5-基)磺酰基]-1H-吲哚-3-基]乙胺
英文名称
WAY-181187
英文别名
2-[1-(6-chloroimidazo[2,1-b][1,3]thiazol-5-yl)sulfonylindol-3-yl]ethanamine;WAY 181187;SAX-187;WAY-181187
Cas No.
554403-49-5
分子式
C15H13N4O2S2Cl
分子量
380.87
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
WAY-181187 (SAX-187) 是一种有效的选择性 5-HT6 受体激动剂,Ki 为 2.2 nM,EC50 为 6.6 nM。WAY181187 介导 5-HT6 受体依赖性信号通路,如 cAMP,Fyn 和 ERK1/2 激酶,作为特异性激动剂。
生物活性
WAY-181187 (SAX-187) is a potent and selective full 5-HT6 receptor agonist with a K i of 2.2 nM and an EC 50 of 6.6 nM. WAY181187 mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist.
性状
Solid
IC50 & Target[1][2]
5-HT6 Receptor 2.2 nM (Ki) 5-HT6 Receptor
体外研究(In Vitro)
WAY181187 (1 and 10 μM) increases activation of ERK1/2. WAY181187 also increases Fyn kinase activity. has not independently confirmed the accuracy of these methods. They are for reference only.Western Blot Analysis
体内研究(In Vivo)
Acute administration of WAY-181187 (3-30 mg/kg, s.c.) significantly increases extracellular GABA concentrations without altering the levels of glutamate or norepinephrine in the rat frontal cortex. Additionally, WAY-181187 (30 mg/kg, s.c.) produces modest yet significant decreases in cortical dopamine and 5-HT levels. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Lee E Schechter, et al. Neuropharmacological Profile of Novel and Selective 5-HT6 Receptor Agonists: WAY-181187 and WAY-208466. Neuropsychopharmacology. 2008 May;33(6):1323-35.
[2]. Teresa Riccioni, et al. ST1936 Stimulates cAMP, Ca2+, ERK1/2 and Fyn Kinase Through a Full Activation of Cloned Human 5-HT6 Receptors. Eur J Pharmacol. 2011 Jul 1;661(1-3):8-14.
溶解度数据
In Vitro: DMSO : 100 mg/mL (262.56 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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