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NRA-0160前沿研究進展

發(fā)布日期：2017-11-13   瀏覽次數(shù)：0
核心提示：NRA-0160 是一種選擇性的 bdopamine D4 receptor/b 拮抗劑，bKsubi/sub/b 值為 0.48 nM；同時對 bdopamine D2 receptor/b，bD3 r
NRA-0160 是一種選擇性的 <b>dopamine D4 receptor</b> 拮抗劑，<b>K<sub>i</sub></b> 值為 0.48 nM；同時對 <b>dopamine D2 receptor</b>，<b>D3 receptor</b>，大鼠 <b>5-HT2A receptor</b> 和 <b>α1 adrenoceptor</b> 分別具有不同程度的親和度，<b>K<sub>i</sub></b> 值分別為 >10000 nM，39 nM，180 nM 和 237 nM。<BR><a href="https://www.medchemexpress.cn/HC-067047.html">HC-067047</a>產(chǎn)品描述：HC-067047 is a potent and selective TRPV4 antagonist with IC50 values of 48 ± 6 nM, 133 ± 25 nM, and 17 ± 3 nM, respectively in human, rat, and mouse. Also inhibits the endogenous TRPV4-mediated response to 4α-PDH (IC50 = 22 nM). target: TRPV4IC 50: 48 ± 6 nM (human), 133 ± 25 nM (rat) , and 17 ± 3 nM (mouse)1) The reference for administration of HC-067047 is 10 mg/kg (i.P)2) HC-067047 caused a significant reduction of the maximal micturition pressure in rats, which might be caused by an effect on TRPV4 in smooth muscle.3) HC-067047 Reduces Pollakisuria and Increases Functional Bladder Capacity4) HC-067047 exhibits high selectivity toward TRPV4: IC50 values were at least 100-fold higher for the closely related channels TRPV1, TRPV2, and TRPV3, and 10-fold higher for TRPM8 and hERG.<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/HC-067047.html">www.medchemexpress.cn/HC-067047.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="">Purity:98%<BR>MWt:439.5207<BR>Formula:C24H23F2N3OS<BR>SMILES:O=C(C1=NC(C2=CC=C(F)C=C2)=C(CCN3CC/C(CC3)=C\C4=CC=CC(F)=C4)S1)N<BR>Pathway:GPCR/G Protein; Neuronal Signaling; <BR>Mechanisms:5-HT Receptor; Adrenergic Receptor; Dopamine Receptor; <BR>Research Area:Neurological Disease<BR>電話： 021-58955995<BR>網(wǎng)址： www.MedChemExpress.cn <BR>地址： 上海市浦東新區(qū)蔡倫路720號2號樓3層
 
 
 
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