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KDR-in-4前沿研究進展

發(fā)布日期：2017-11-13   瀏覽次數(shù)：0
核心提示：KDR-in-4 是有效的激酶插入結(jié)構(gòu)域受體 (bKDR/VEGFR2/b) 抑制劑，bICsub50/sub/b 值為7 nM。BRa href=https://www.medchemexpress
KDR-in-4 是有效的激酶插入結(jié)構(gòu)域受體 (<b>KDR/VEGFR2</b>) 抑制劑，<b>IC<sub>50</sub></b> 值為7 nM。<BR><a href="https://www.medchemexpress.cn/SCH-546738.html">SCH 546738</a>產(chǎn)品描述：SCH 546738 is a novel, potent and non-competitive <b>CXCR3</b> antagonist, the affinity constant (<b>K<sub>i</sub></b>) of SCH 546738 binding to human CXCR3 receptor is determined to be 0.4 nM in multiple experiments.IC50 & Target: Ki: 0.4 nM (CXCR3 receptor)<sup>[1]</sup><i><b>In Vitro:</b></i> The affinity of SCH 546738 binding to human CXCR3 receptor is determined by competition binding analysis using <sup>35</sup>S radiolabeled SCH 535390 (a sulfonamide analog of the CXCR3 compound series with a K<sub>d</sub> of 0.6 nM) as a competitive tracer. In addition, SCH 546738 displaces radiolabeled CXCL10 and CXCL11 from human CXCR3 with IC<sub>50</sub> ranging from 0.8 to 2.2 nM in a non-competitive manner. SCH 546738 potently and specifically inhibits CXCR3-mediated chemotaxis in human activated T cells with IC<sub>90</sub> about 10 nM. Competition of human CXCL10 and CXCL11 binding to human CXCR3 by SCH 546738 is determined at various concentrations of [<sup>125</sup>I]hCXCL10 an<br><br><br><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)域的一流供應商， 產(chǎn)品涵蓋癌癥、神經(jīng)科學、抗感染、表觀遺傳學等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。</span><br style="color: rgb(62,62,62);font-family: "Helvetica Neue" , Helvetica , Arial , sans-serif;font-size: 11.818182px;line-height: 22.0px;background-color: rgb(251,251,251);"><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);">MCE 對每批產(chǎn)品都進行嚴格的LCMS和NMR檢驗，其產(chǎn)品已被全球近萬名客戶廣泛使用并發(fā)表大量文章、專利；</span><br style="color: rgb(62,62,62);font-family: "Helvetica Neue" , Helvetica , Arial , sans-serif;font-size: 11.818182px;line-height: 22.0px;background-color: rgb(251,251,251);"><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);">MCE 定期增加各領(lǐng)域熱門抑制劑、激動劑，不斷擴增已有化合物庫，以滿足最新的科研需求；</span><br style="color: rgb(62,62,62);font-family: "Helvetica Neue" , Helvetica , Arial , sans-serif;font-size: 11.818182px;line-height: 22.0px;background-color: rgb(251,251,251);"><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);">數(shù)千種產(chǎn)品在上海有充足備貨，24-48小時內(nèi)送達客戶；</span><br style="color: rgb(62,62,62);font-family: "Helvetica Neue" , Helvetica , Arial , sans-serif;font-size: 11.818182px;line-height: 22.0px;background-color: rgb(251,251,251);"><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);">大量產(chǎn)品提供免費試用裝；</span><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);">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/SCH-546738.html">www.medchemexpress.cn/SCH-546738.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" alt="">Purity:98%<BR>MWt:391.4629<BR>Formula:C23H25N3O3<BR>SMILES:O=C1NC2=C(C=CC=C2)C=C1C(N3)=CC4=C3C=CC(OCCN(CCOC)C)=C4<BR>Pathway:Protein Tyrosine Kinase/RTK; <BR>Mechanisms:VEGFR; <BR>Research Area:Cardiovascular Disease<BR>電話： 021-58955995<BR>網(wǎng)址： www.MedChemExpress.cn <BR>地址： 上海市浦東新區(qū)蔡倫路720號2號樓3層
 
 
 
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