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Merck
CN

PZ0135

Sigma-Aldrich

PHA-543613

≥98% (HPLC)

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别名:
N- [(3R)-1-氮杂双环 [2.2.2] 辛-3-基] 呋喃 [2,3-c] 吡啶-5-甲酰胺
经验公式(希尔记法):
C15H17N3O2
分子量:
271.31
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77

质量水平

检测方案

≥98% (HPLC)

形式

powder

颜色

white to off-white

溶解性

DMSO: ≥20 mg/mL

储存温度

room temp

SMILES字符串

O=C(N[C@H]1CN2CC[C@H]1CC2)c3cc4ccoc4cn3

InChI

1S/C15H17N3O2/c19-15(12-7-11-3-6-20-14(11)8-16-12)17-13-9-18-4-1-10(13)2-5-18/h3,6-8,10,13H,1-2,4-5,9H2,(H,17,19)/t13-/m0/s1

InChI key

IPKZCLGGYKRDES-ZDUSSCGKSA-N

基因信息

human ... CHRNA7(1139)

应用

PHA-543613已被用于研究其在接受β-淀粉样蛋白(Aβ)25-35-治疗小鼠中识别记忆和神经血管偶联(NVC)反应中的作用。它还被用于研究其对小鼠中Aβ25-35诱导的受体改变和认知障碍的影响。

生化/生理作用

PHA-543613 是一种强效选择性 α⑦nAChR 激动剂。烟碱型乙酰胆碱受体是由烟碱激活的配体门控离子通道,在多组织中表达,在脑内有较高的功能表达。同源亚型 α7 是精神分裂症和阿尔茨海默病认知缺陷的潜在治疗靶点。PHA-543613 在 体外 (结合、钙通量、膜片钳)和 体内 (听觉门控、新物体识别)试验中均具有活性。
PHA-543613具有快速的脑部渗透特性。

特点和优势

该化合物在《受体分类和信号转导》手册的 乙酰胆碱受体(烟碱) 页面上有详细描述。想要浏览手册的其他页面, 请单击此处

WGK

WGK 1

闪点(°F)

Not applicable

闪点(°C)

Not applicable


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Mark R Albertini et al.
Environmental and molecular mutagenesis, 49(9), 676-687 (2008-08-21)
The identification of specific lymphocyte populations that mediate tumor immune responses is required for elucidating the mechanisms underlying these responses and facilitating therapeutic interventions in humans with cancer. To this end, mutant hypoxanthine-guanine phosphoribosyltransferase (HPRT) deficient (HPRT-) T-cells were used
Stefan M Gold et al.
Journal of neuroinflammation, 5, 32-32 (2008-08-02)
Multiple sclerosis is a chronic inflammatory disease of the central nervous system with a pronounced neurodegenerative component. It has been suggested that novel treatment options are needed that target both aspects of the disease. Evidence from basic and clinical studies
Effect of alpha-7 nicotinic acetylcholine receptor activation on beta-amyloid induced recognition memory impairment. Possible role of neurovascular function
Sadigh-Eteghad S, et al.
Acta Cirurgica Brasileira / Sociedade Brasileira Para Desenvolvimento Pesquisa em Cirurgia, 30(11), 736-742 (2015)
Selective activation of $\alpha$7 nicotinic acetylcholine receptor by PHA-543613 improves A$\beta$25--35-mediated cognitive deficits in mice
Sadigh-Eteghad S, et al.
Neuroscience, 298(11), 81-93 (2015)
Cleber A Trujillo et al.
EMBO molecular medicine, 13(1), e12523-e12523 (2021-01-28)
Duplication or deficiency of the X-linked MECP2 gene reliably produces profound neurodevelopmental impairment. MECP2 mutations are almost universally responsible for Rett syndrome (RTT), and particular mutations and cellular mosaicism of MECP2 may underlie the spectrum of RTT symptomatic severity. No

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