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CYM-5541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/CYM-5541.htmlCYM-5541/a產(chǎn)品描述：CYM-5541 (ML249) is an selective and allosteric b
<a href="https://www.medchemexpress.com/CYM-5541.html">CYM-5541</a>產(chǎn)品描述：CYM-5541 (ML249) is an selective and allosteric <b>S1P<sub>3</sub></b> receptor agonist with an <b>EC<sub>50</sub></b> between 72 and 132 nM.

IC50 & Target: EC50: between 72 and 132 nM (S1P<sub>3</sub>)<sup>[1]</sup>

<i><b>In Vitro:</b></i> CYM-5541 is a full agonist, able to reach the maximum level of ERK phosphorylation that is observed with S1P. CYM-5541 has an EC<sub>50</sub> of between 72 and 132 nM and exhibits exquisite selectivity over other S1P receptor subtypes: S1P1 EC<sub>50</sub>>10 μM, S1P2 EC<sub>50</sub>>50 μM, S1P4 EC<sub>50</sub>>50 μM, and S1P5 EC<sub>50</sub>>25 μM. CYM-5541 also shows selectivity over a large panel of protein targets, with no significant activities, in the Ricerca profiling panel of 55 GPCRs, ion channels, and transporters. CYM-5541 allowed us to identify an allosteric site wher F263 is a key gate-keeper residue for its affinity and efficacy. The novel allosteric hydrophobic pocket may account for the S1P3 selectivity of CYM-5541<sup>[1]</sup>.<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(kù)。</span><br><br>產(chǎn)品鏈接：<a href="http://www.medchemexpress.cn/cym-5541.html">www.medchemexpress.cn/cym-5541.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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