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Olcegepant研究進展

發(fā)布日期：2017-10-27   瀏覽次數：0
核心提示：a href=https://www.medchemexpress.com/Olcegepant.htmlOlcegepant/a產品描述：Olcegepant is the first potent and selective
<a href="https://www.medchemexpress.com/Olcegepant.html">Olcegepant</a>產品描述：Olcegepant is the first potent and selective non-peptide antagonist of the <b>calcitonin gene-related peptide 1 (CGRP1) receptor</b> with <b>IC<sub>50</sub></b> of 0.03 nM and with a <b>K<sub>i</sub></b> of 14.4 pM for human CGRP.

IC50 & Target: IC50: 0.03 nM (CGRP1)<sup>[1]</sup><br/>

Ki: 14.4 pM (hCGRP)<sup>[2]</sup>

<i><b>In Vitro:</b></i> Olcegepant possesses higher affinity for the human CGRP receptor than the endogenous ligand CGRP and 150-fold higher affinity compared to the peptidic antagonist CGRP8-37. Olcegepant reverses CGRP-mediated vasodilation in human cerebral vessels and inhibits neurogenic vasodilation in a surrogate animal model of migraine pathophysiology<sup>[1]</sup>. Olcegepant (BIBN4096BS) is extremely potent at primate CGRP receptors exhibiting an affinity (K<sub>i</sub>) for human CGRP receptors of 14.4±6.3 (n=4) pM<sup>[2]</sup>. Several lines of evidence suggest that a calcitonin-gene related peptide (CGRP) receptor antagonist may serve as a novel abortiv<br><br>
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<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、激動劑、API及化合物庫，總部位于美國新澤西，分別在瑞典和上海設有歐洲區(qū)子公司和亞洲區(qū)總代理，營銷網點遍及全球20多個國家地區(qū)。MCE經過多年努力已成為全球生物活性小分子領域的一流供應商， 產品涵蓋癌癥、神經科學、抗感染、表觀遺傳學等20個熱門研究領域，PI3K、MAPK等近千個細分靶點，超過4000個活性小分子化合物現貨，以及GPCR、API、離子通道等超過20種不同類型的化合物庫，同時提供從毫克到千克的專業(yè)定制合成服務。</span>
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已為全球多個知名企業(yè)、院校構建各種定制型化合物庫。</span><br><br>產品鏈接：<a href="http://www.medchemexpress.cn/olcegepant.html">www.medchemexpress.cn/olcegepant.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"

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