當(dāng)前位置: 首頁(yè) » 資訊 » 行業(yè)動(dòng)態(tài) » 正文

RG-12525前沿研究進(jìn)展

發(fā)布日期：2017-11-13   瀏覽次數(shù)：0
核心提示：RG-12525 是一種特異性的，競(jìng)爭(zhēng)性的，可口服的 LTC4，LTD4 和 LTE4 拮抗劑，也是 bPPAR-/b 的激動(dòng)劑，bICsub50/sub/b 值約為 60
RG-12525 是一種特異性的，競(jìng)爭(zhēng)性的，可口服的 LTC4，LTD4 和 LTE4 拮抗劑，也是 <b>PPAR-γ</b> 的激動(dòng)劑，<b>IC<sub>50</sub></b> 值約為 60 nM，<b>CYP3A4</b> 的抑制劑， K<sub>i</sub> 值為 0.5 µM。<BR><a href="https://www.medchemexpress.cn/9-Aminocamptothecin.html">9-Aminocamptothecin</a>產(chǎn)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);">公司介紹：MedChemExpress(MCE)專(zhuān)注于各種抑制劑、激動(dòng)劑、API及化合物庫(kù)，總部位于美國(guó)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(yíng)銷(xiāo)網(wǎng)點(diǎn)遍及全球20多個(gè)國(guó)家地區(qū)。MCE經(jīng)過(guò)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(gè)熱門(mén)研究領(lǐng)域，PI3K、MAPK等近千個(gè)細(xì)分靶點(diǎn)，超過(guò)4000個(gè)活性小分子化合物現(xiàn)貨，以及GPCR、API、離子通道等超過(guò)20種不同類(lèi)型的化合物庫(kù)，同時(shí)提供從毫克到千克的專(zhuān)業(yè)定制合成服務(wù)。</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(duì)每批產(chǎn)品都進(jìn)行嚴(yán)格的LCMS和NMR檢驗(yàn)，其產(chǎn)品已被全球近萬(wàn)名客戶(hù)廣泛使用并發(fā)表大量文章、專(zhuān)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(mén)抑制劑、激動(dòng)劑，不斷擴(kuò)增已有化合物庫(kù)，以滿(mǎn)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(shí)內(nèi)送達(dá)客戶(hù)；</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(fèi)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(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/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>電話(huà)： 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(hào)2號(hào)樓3層
 
 
 
?