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ICA-069673研究進(jìn)展

發(fā)布日期：2017-10-30   瀏覽次數(shù)：0
核心提示：a href=https://www.medchemexpress.com/ICA-069673.htmlICA-069673/a產(chǎn)品描述：ICA-069673 is a bKCNQ2/Q3/b potassium channel
<a href="https://www.medchemexpress.com/ICA-069673.html">ICA-069673</a>產(chǎn)品描述：ICA-069673 is a <b>KCNQ2/Q3</b> potassium channel activator with an <b>IC<sub>50</sub></b> of 0.69 μM.

IC50 & Target: IC50: 0.69 μM (KCNQ2/Q3 potassium channel)<sup>[1]</sup>

<i><b>In Vitro:</b></i> ICA-069673 is found to be 20-fold selective for KCNQ2/Q3 over KCNQ3/Q5 and has no measurable activity against a panel of cardiac ion channels (IC<sub>50</sub> values > 30 μM for hERG, Nav1.5, L type channels, and KCNQ1) as well as no activity on GABA(A) gated channels at 10 μM<sup>[1]</sup>. ICA-069673 exhibits much stronger effects on KCNQ2 channels, including a large hyperpolarizing shift of the voltage-dependence of activation, an 2-fold enhancement of peak current and pronounced subtype specificity for KCNQ2 over KCNQ3. based on ICA73 sensitivity of chimeric constructs of the transmembrane segments of KCNQ2 and KCNQ3, this drug appears to interact with the KCNQ2 voltage sensor (S1-S4)<sup>[2]</sup>.

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已為全球多個知名企業(yè)、院校構(gòu)建各種定制型化合物庫。</span><br><br>產(chǎn)品鏈接：<a href="http://www.medchemexpress.cn/ica-069673.html">www.medchemexpress.cn/ica-069673.html</a><br><br></span><img style="width: 600.0px;height: 310.0px;"

src="http://img.dxycdn.com/trademd/upload/userfiles/image/2014/08/A1408605159png_small.jpg"

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