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RG-12525前沿研究进展

发布日期:2017-11-13   浏览次数:0
核心提示:RG-12525 是一种特异性的,竞争性的,可口服的 LTC4,LTD4 和 LTE4 拮抗剂,也是 bPPAR-/b 的激动剂,bICsub50/sub/b 值约为 60
RG-12525 是一种特异性的,竞争性的,可口服的 LTC4,LTD4 和 LTE4 拮抗剂,也是 <b>PPAR-γ</b> 的激动剂,<b>IC<sub>50</sub></b> 值约为 60 nM,<b>CYP3A4</b> 的抑制剂, K<sub>i</sub> 值为 0.5 µM。<BR><a href="https://www.medchemexpress.cn/9-Aminocamptothecin.html">9-Aminocamptothecin</a>产品描述:9-Aminocamptothecin is a <b>topoisomerase I</b> inhibitor with potent anticancer activity.IC50 & Target: Topoisomerase<sup>[1]</sup><i><b>In Vitro:</b></i> In human breast (MCF-7), bladder (MGH-U1), and colon (HT-29) cancer cell lines, 9-Aminocamptothecin cytotoxicity increases with both higher drug concentrations and longer exposure times. Minimal cell killing is also observed unless 9-Aminocamptothecin concentrations exceeds a threshold of 2.7 nm<sup>[1]</sup>. 9-Aminocamptothecin inhibits PC-3, PC-3M, DU145, and LNCaP cells with IC<sub>50</sub> values of 34.1, 10, 6.5, and 8.9 nM, respectively after 96 h of drug exposure<sup>[2]</sup>.<i><b>In Vivo:</b></i> 9-Aminocamptothecin inhibits tumor growth at the lowest oral dose (0.35 mg/kg/day), wheras higher oral doses (0.75 and 1 mg/kg/day) and s.c. administration (4 mg/kg/week) causes tumor regression. 9-Aminocamptothecin is well tolerated at all doses, with no toxic death or weight loss of more than 10% observed in any group<s<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/9-Aminocamptothecin.html">www.medchemexpress.cn/9-Aminocamptothecin.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:423.4665<BR>Formula:C25H21N5O2<BR>SMILES:C1(COC2=CC=C(OCC3=CC=CC=C3CC4=NN=NN4)C=C2)=NC5=CC=CC=C5C=C1<BR>Pathway:Cell Cycle/DNA Damage; GPCR/G Protein; metabolic Enzyme/Protease; NF-κB; <BR>Mechanisms:Cytochrome P450; Leukotriene Receptor; PPAR; <BR>Research Area:metabolic 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