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PF-01247324研究進展

發(fā)布日期：2017-10-30   瀏覽次數(shù)：0
核心提示：a href=https://www.medchemexpress.com/PF-01247324.htmlPF-01247324/a產(chǎn)品描述：PF-01247324 is a selective and orally bioav
<a href="https://www.medchemexpress.com/PF-01247324.html">PF-01247324</a>產(chǎn)品描述：PF-01247324 is a selective and orally bioavailable <b>Na<sub>v</sub>1.8</b> channel blocker with an <b>IC<sub>50</sub></b> of 196 nM for recombinant human Na<sub>v</sub>1.8 channel.

IC50 & Target: IC50: 196 nM (hNa<sub>v</sub>1.8)<sup>[1]</sup>

<i><b>In Vitro:</b></i> PF-01247324 inhibits native tetrodotoxin-resistant (TTX-R) currents in human dorsal root ganglion (DRG) neurons (IC<sub>50</sub>=331 nM) and in recombinantly expressed h Na<sub>v</sub>1.8 channels (IC<sub>50</sub>=196 nM), with 50-fold selectivity over recombinantly expressed TTX-R hNav1.5 channels (IC<sub>50</sub>=10 μM) and 65-100-fold selectivity over TTX-sensitive (TTX-S) channels (IC<sub>50</sub>=10-18 μM). <i>In vitro</i> current clamp shows that PF-01247324 reduces excitability in both rat and human DRG neurons and also alters the waveform of the action potential<sup>[1]</sup>.

<i><b>In Vivo:</b></i> Experiments n rodents demonstrates efficacy in both inflammatory and neuropathic pain models. PF-01247324 redu<br><br>
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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(chǎn)品鏈接：<a href="http://www.medchemexpress.cn/pf-01247324.html">www.medchemexpress.cn/pf-01247324.html</a><br><br></span><img style="width: 600.0px;height: 310.0px;"

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