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KDR-in-4前沿研究进展

发布日期：2017-11-13   浏览次数：0
核心提示：KDR-in-4 是有效的激酶插入结构域受体 (bKDR/VEGFR2/b) 抑制剂，bICsub50/sub/b 值为7 nM。BRa href=https://www.medchemexpress
KDR-in-4 是有效的激酶插入结构域受体 (<b>KDR/VEGFR2</b>) 抑制剂，<b>IC<sub>50</sub></b> 值为7 nM。<BR><a href="https://www.medchemexpress.cn/SCH-546738.html">SCH 546738</a>产品描述：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);">公司介绍：MedChemExpress(MCE)专注于各种抑制剂、激动剂、API及化合物库，总部位于美国新泽西，分别在瑞典和上海设有欧洲区子公司和亚洲区总代理，营销网点遍及全球20多个国家地区。MCE经过多年努力已成为全球生物活性小分子领域的一流供应商， 产品涵盖癌症、神经科学、抗感染、表观遗传学等20个热门研究领域，PI3K、MAPK等近千个细分靶点，超过4000个活性小分子化合物现货，以及GPCR、API、离子通道等超过20种不同类型的化合物库，同时提供从毫克到千克的专业定制合成服务。</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 对每批产品都进行严格的LCMS和NMR检验，其产品已被全球近万名客户广泛使用并发表大量文章、专利；</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 定期增加各领域热门抑制剂、激动剂，不断扩增已有化合物库，以满足最新的科研需求；</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);">数千种产品在上海有充足备货，24-48小时内送达客户；</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);">大量产品提供免费试用装；</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);">已为全球多个知名企业、院校构建各种定制型化合物库。</span><br><br>产品链接：<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>电话： 021-58955995<BR>网址： www.MedChemExpress.cn <BR>地址： 上海市浦东新区蔡伦路720号2号楼3层