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Olcegepant (hydrochloride)研究进展

发布日期：2017-10-27   浏览次数：0
核心提示：a href=https://www.medchemexpress.com/Olcegepant__hydrochloride_.htmlOlcegepant (hydrochloride)/a产品描述：Olcegepant hy
<a href="https://www.medchemexpress.com/Olcegepant__hydrochloride_.html">Olcegepant (hydrochloride)</a>产品描述：Olcegepant hydrochloride 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<br><br>
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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/olcegepant-hydrochloride.html">www.medchemexpress.cn/olcegepant-hydrochloride.html</a><br><br></span><img style="width: 600.0px;height: 310.0px;"

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