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MLi-2

發(fā)布日期:2017-10-26   瀏覽次數(shù):0
核心提示:a href=https://www.medchemexpress.com/MLi-2.htmlMLi-2/a產(chǎn)品描述:MLi-2 is an a potent, highly selective, orally availabl
<a href="https://www.medchemexpress.com/MLi-2.html">MLi-2</a>產(chǎn)品描述:MLi-2 is an a potent, highly selective, orally available, brain penetrant inhibitor of <b>LRRK2</b> with an <b>IC<sub>50</sub></b> of 0.76 nM.

IC50 & Target: IC50: 0.76 nM (LRRK2)<sup>[1]</sup>

<i><b>In Vitro:</b></i> MLi-2 exhibits exceptional potency in a purified LRRK2 kinase assay <i>in vitro</i>( IC<sub>50</sub>=0.76 nM), a cellular assay monitoring dephosphorylation of LRRK2 pSer935 LRRK2 (IC<sub>50</sub>=1.4 nM), and a radioligand competition binding assay (IC<sub>50</sub>=3.4 nM). MLi-2 has greater than 295-fold selectivity for over 300 kinases in addition to a diverse panel of receptors and ion channels<sup>[1]</sup>.

<i><b>In Vivo:</b></i> Acute oral and subchronic dosing in MLi-2 mice results in dose-dependent central and peripheral target inhibition over a 24-hour period as measured by dephosphorylation of pSer935 LRRK2. Treatment of MitoPark mice with MLi-2 is well tolerated over a 15-week period at brain and plasma exposures. Morphologic changes in the lung, consiste<br><br>
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<span style="outline: 0.0px;line-height: 22.0px;color: rgb(62,62,62);font-family: "Helvetica Neue" , Helvetica , Arial , sans-serif;font-size: 11.818182px;background-color: rgb(251,251,251);">公司介紹:MedChemExpress(MCE)專注于各種抑制劑、激動劑、API及化合物庫,總部位于美國新澤西,分別在瑞典和上海設(shè)有歐洲區(qū)子公司和亞洲區(qū)總代理,營銷網(wǎng)點遍及全球20多個國家地區(qū)。MCE經(jīng)過多年努力已成為全球生物活性小分子領(lǐng)域的一流供應(yīng)商, 產(chǎn)品涵蓋癌癥、神經(jīng)科學(xué)、抗感染、表觀遺傳學(xué)等20個熱門研究領(lǐng)域,PI3K、MAPK等近千個細分靶點,超過4000個活性小分子化合物現(xiàn)貨,以及GPCR、API、離子通道等超過20種不同類型的化合物庫,同時提供從毫克到千克的專業(yè)定制合成服務(wù)。</span>
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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/mli-2.html">www.medchemexpress.cn/mli-2.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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