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NRA-0160前沿研究进展

发布日期：2017-11-13   浏览次数：0
核心提示：NRA-0160 是一种选择性的 bdopamine D4 receptor/b 拮抗剂，bKsubi/sub/b 值为 0.48 nM；同时对 bdopamine D2 receptor/b，bD3 r
NRA-0160 是一种选择性的 <b>dopamine D4 receptor</b> 拮抗剂，<b>K<sub>i</sub></b> 值为 0.48 nM；同时对 <b>dopamine D2 receptor</b>，<b>D3 receptor</b>，大鼠 <b>5-HT2A receptor</b> 和 <b>α1 adrenoceptor</b> 分别具有不同程度的亲和度，<b>K<sub>i</sub></b> 值分别为 >10000 nM，39 nM，180 nM 和 237 nM。<BR><a href="https://www.medchemexpress.cn/HC-067047.html">HC-067047</a>产品描述：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);">公司介绍：MedChemExpress(MCE)专注于各种抑制剂、激动剂、API及化合物库，总部位于美国新泽西，分别在瑞典和上海设有欧洲区子公司和亚洲区总代理，营销网点遍及全球20多个国家地区。MCE经过多年努力已成为全球生物活性小分子领域的一流供应商， 产品涵盖癌症、神经科学、抗感染、表观遗传学等20个热门研究领域，PI3K、MAPK等近千个细分靶点，超过4000个活性小分子化合物现货，以及GPCR、API、离子通道等超过20种不同类型的化合物库，同时提供从毫克到千克的专业定制合成服务。</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 对每批产品都进行严格的LCMS和NMR检验，其产品已被全球近万名客户广泛使用并发表大量文章、专利；</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 定期增加各领域热门抑制剂、激动剂，不断扩增已有化合物库，以满足最新的科研需求；</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);">数千种产品在上海有充足备货，24-48小时内送达客户；</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);">大量产品提供免费试用装；</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/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>电话： 021-58955995<BR>网址： www.MedChemExpress.cn <BR>地址： 上海市浦东新区蔡伦路720号2号楼3层