當(dāng)前位置: 首頁 » 資訊 » 行業(yè)動態(tài) » 正文

BAR502研究進展

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>
<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(shè)有歐洲區(qū)子公司和亞洲區(qū)總代理，營銷網(wǎng)點遍及全球20多個國家地區(qū)。MCE經(jīng)過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個熱門研究領(lǐng)域，PI3K、MAPK等近千個細分靶點，超過4000個活性小分子化合物現(xiàn)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(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 對每批產(chǎn)品都進行嚴(yán)格的LCMS和NMR檢驗，其產(chǎn)品已被全球近萬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、激動劑，不斷擴增已有化合物庫，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小時內(nèi)送達客戶；</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);">
已為全球多個知名企業(yè)、院校構(gòu)建各種定制型化合物庫。</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;"

src="http://img.dxycdn.com/trademd/upload/userfiles/image/2014/08/A1408605159png_small.jpg"

alt="">
 
 
 
?