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BAR502研究進(jìn)展

發(fā)布日期：2017-10-27   瀏覽次數(shù)：0
核心提示：a href=https://www.medchemexpress.com/BAR502.htmlBAR502/a產(chǎn)品描述：BAR502 is a dual bFXR/b and bGPBAR1/b agonist with bI
<a href="https://www.medchemexpress.com/BAR502.html">BAR502</a>產(chǎn)品描述：BAR502 is a dual <b>FXR</b> and <b>GPBAR1</b> agonist with <b>IC<sub>50</sub></b> values of 2 μM and 0.4 μM, respectively.

IC50 & Target: IC50: 2 μM (FXR), 0.4 μM (GPBAR1)<sup>[1]</sup>

<i><b>In Vitro:</b></i> BAR502 is a truncated side chain alcohol with both substituents on ring B in α-configuration. At the concentration of 10 μM, BAR502 fails to transactivate GR, PPARγ, and LXR, respectively, but it transactivates the nuclear receptor PXR. BAR502 is able to induce the expression of pro-glucagon mRNA in GLUTAg cells, an intestinal endocrine cell line, as well as to increase cAMP concentrations in THP-1 cells. BAR502 induces the expression of OSTα, BSEP, and SHP in HepG2 cells. BAR502 shows a very potent activity in the recruitment of SRC-1 coactivator and high affinity to FXR<sup>[1]</sup>.

<i><b>In Vivo:</b></i> Treatment with BAR502 causes a 10% reduction of b.w., increases insulin sensitivity and circulating levels of HDL, while reduces steatosis, inflammatory and fibrosis sco<br><br>
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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/bar502.html">www.medchemexpress.cn/bar502.html</a><br><br></span><img style="width: 600.0px;height: 310.0px;"

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