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TB5研究進(jìn)展

發(fā)布日期:2017-10-27   瀏覽次數(shù):0
核心提示:a href=https://www.medchemexpress.com/TB5.htmlTB5/a產(chǎn)品描述:TB5 is a potent, selective and reversible inhibitor of bhMA
<a href="https://www.medchemexpress.com/TB5.html">TB5</a>產(chǎn)品描述:TB5 is a potent, selective and reversible inhibitor of <b>hMAO-B</b> with a <b>K<sub>i</sub></b> value of 0.11±0.01 μM.

IC50 & Target: Ki: 0.11±0.01 μM (hMAO-B)<sup>[1]</sup>

<i><b>In Vitro:</b></i> TB5 and TB8 interacts with the catalytic site of hMAO-B and hMAO-A with a competitive mode of inhibition. TB5 shows the best inhibitory activity and higher selectivity toward hMAO-B, with K<sub>i</sub> and SI values of 0.11±0.01μM and 13.18, respectively. hMAO-B inhibition by compound TB5 and hMAO-A inhibition by compound TB8 are completely reversed after 24 h of dialysis. Cytotoxicity studies show TB5 is nontoxic at 5 and 25 μM, resulting in cell viabilities of 95.75% and 84.59 %, respectively<sup>[1]</sup>.

<i><b>In Vivo:</b></i> Compounds are dissolved in DMSO (5 mg/mL) and diluted with PBS/EtOH (70:30).Kinetic analyses are carried out for TB5 and TB8. A set of Lineweaver–Burk plots are constructed in the absence and presence of various concentrations of compounds TB5 and TC8. The se<br><br>
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已為全球多個(gè)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/tb5.html">www.medchemexpress.cn/tb5.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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