MHP 是 <b>SPHK1</b> 的激活劑,能夠刺激 KC細(xì)胞中 CAMP mRNA 的表達(dá)和蛋白的產(chǎn)生。<BR><a href="https://www.medchemexpress.cn/CPI-1205.html">CPI-1205</a>產(chǎn)品描述:CPI-1205, a highly potent and selective <b>EZH2</b> inhibitor (biochemical <b>IC<sub>50</sub></b>=2 nM, cellular <b>EC<sub>50</sub></b>=32 nM). IC50 & Target: IC50: 2 nM (EZH2)<sup>[1]</sup><i><b>In Vitro:</b></i> When tested within an in vitro hERG binding assay at concentration ranges of 45 nM to 100 μM, CPI-1205 shows an IC<sub>50</sub> of 21.3 μM. CPI-1205 demonstrates modest selectivity (EZH1 IC<sub>50</sub> of 52±11 nM) when tested against enhancer of zeste homologue 1 (EZH1), a methyltransferase highly related to EZH2. CPI-1205 achieves unbound exposures well above their respective cellular potencies; however, only the unbound exposure for CPI-1205 remains well above the cellular EC<sub>50</sub> up to 4 h<sup>[1]</sup>. <i><b>In Vivo:</b></i> CPI-1205 is dosed at 160 mg/kg orally twice daily (po BID) for 25 days in tumor bearing female CB-17 SCID mice. Upon treatment of tumor-bearing CB-17 SCID mice with CPI-1205, tumor regression is observed within 2 weeks. By the end of<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(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)銷網(wǎng)點(diǎn)遍及全球20多個(gè)國(guó)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(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)熱門研究領(lǐng)域,PI3K、MAPK等近千個(gè)細(xì)分靶點(diǎn),超過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20種不同類型的化合物庫(kù),同時(shí)提供從毫克到千克的專業(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(dòng)劑,不斷擴(kuò)增已有化合物庫(kù),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(shí)內(nèi)送達(dá)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(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/CPI-1205.html">www.medchemexpress.cn/CPI-1205.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:293.3581<BR>Formula:C16H23NO4<BR>SMILES:OC(C=C1)=CC=C1C[C@@H](C(OC)=O)NC(CCCCC)=O<BR>Pathway:Immunology/Inflammation; <BR>Mechanisms:SPHK; <BR>Research Area:Others<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(hào)2號(hào)樓3層 |
MHP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:MHP 是 bSPHK1/b 的激活劑,能夠刺激 KC細(xì)胞中 CAMP mRNA 的表達(dá)和蛋白的產(chǎn)生。BRa href=https://www.medchemexpress.cn/CPI-120
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