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Darbufelone (mesylate)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/Darbufelone_(mesylate).htmlDarbufelone (mesylate)/a產(chǎn)品描述：Darbufelone mesylate
<a href="https://www.medchemexpress.com/Darbufelone_(mesylate).html">Darbufelone (mesylate)</a>產(chǎn)品描述：Darbufelone mesylate is a dual inhibitor of cellular <b>prostaglandin</b> and <b>leukotriene</b> production. Darbufelone potently inhibits <b>PGHS-2</b> (<b>IC<sub>50</sub></b> = 0.19 μM) but is much less potent with <b>PGHS-1</b> (<b>IC<sub>50</sub></b>= 20 μM).

IC50 & Target: IC50: 0.19 μM (PGHS-2), 20 μM (PGHS-1)<sup>[1]</sup>

<i><b>In Vitro:</b></i> Darbufelone is a noncompetitive inhibitor of PGHS-2 (K<sub>i</sub>=10±5 μM). Darbufelone quenches the fluorescence of PGHS-2 at 325 nm (lambda(ex)=280 nm) with K<sub>d</sub>=0.98±0.03 μM<sup>[1]</sup>.To test the putative anti-proliferative effect of Darbufelone, A549, H520 and H460 cell lines are used, which are established from three distinct pathological subtypes of NSCLC (adenocarcinoma, squamous and large cell lung cancer respectively). Increasing concentrations of Darbufelone, ranging from 5 to 60 μM, are tested for 72 h. The cell growth inhibition of these three cell lines gradually increases with higher drug concentration. T<br><br>
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