| Bamirastine 抑制配體結(jié)合到重組人組胺 H<sub>1</sub> 受體 (<b>rhH<sub>1</sub>R</b>)，<b>IC<sub>50</sub></b> 為 17.3 nM。<BR><a href="https://www.medchemexpress.cn/Semagacestat.html">Semagacestat</a>產(chǎn)品描述：Semagacestat is a <b>γ-secretase</b> inhibitor, inhibits <b>β-amyloid</b> (<b>Aβ42</b>), <b>Aβ38</b> and <b>Aβ40</b> with <b>IC<sub>50</sub></b> of 10.9, 12 and 12.1 nM, respectively; also inhibits <b>Notch</b> signaling with <b>IC<sub>50</sub></b> of 14.1 nM. IC50 & Target: IC50: 10.9 nM (Aβ42), 12 nM (Aβ38), 12.1 nM (Aβ40), 14.1 nM (Notch)<sup>[1]</sup><i><b>In Vitro:</b></i> Semagacestat (LY450139) reduces the secretion of Aβ42, Aβ40, and Aβ38 in 96-well-cultured media and increases β-CTF in cell lysates as expected, although this increase is unexpectedly attenuated at high concentrations<sup>[1]</sup>. In cortical neurons (CTX), Semagacestat (LY450139) causes a concentration-dependent decrease in Aβ40 secreted into the medium with IC<sub>50</sub> value 111 nM for Semagacestat. Semagacestat causes a concentration-dependent decrease in Aβ40 and Aβ42 secreted into the medium with an IC<sub>50</sub> value of 126 and 130 nM, respectively<sup>[2]</sup>.<i><b>In Vivo:</b></i> Semag<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(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/Semagacestat.html">www.medchemexpress.cn/Semagacestat.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:527.6572<BR>Formula:C31H37N5O3<BR>SMILES:O=C(O)C(C)(C)C1=CN2N=C(NCCCN3CCC(OC(C4=CC=CC=C4)C5=CC=CC=C5)CC3)C=CC2=N1<BR>Pathway:GPCR/G Protein; Immunology/Inflammation; <BR>Mechanisms:Histamine Receptor; <BR>Research Area:Inflammation/Immunology<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 |
Bamirastine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：Bamirastine 抑制配體結(jié)合到重組人組胺 Hsub1/sub 受體 (brhHsub1/subR/b)，bICsub50/sub/b 為 17.3 nM。BRa href=https://www.m
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