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ABT-639 (hydrochloride)前沿研究進展

發(fā)布日期：2017-11-13   瀏覽次數(shù)：0
核心提示：ABT-639 hydrochloride 是一種新型選擇性的 T 型 bCasup2+/sup/b 通道阻滯劑。BRa href=https://www.medchemexpress.cn/Taranaba
ABT-639 hydrochloride 是一種新型選擇性的 T 型 <b>Ca<sup>2+</sup></b> 通道阻滯劑。<BR><a href="https://www.medchemexpress.cn/Taranabant.html">Taranabant</a>產(chǎn)品描述：Taranabant is a highly potent and selective <b>cannabinoid 1</b> (<b>CB1</b>) receptor inverse agonist that inhibits the binding and functional activity of various agonists, with a binding <b>K<sub>i</sub></b> of 0.13 nM for the human CB1R in vitro. IC50 & Target: IC50: 0.3 nM (hCB1R), 0.4 nM (rCB1R)<sup>[1]</sup><br/>Ki: 0.13 nM (hCB1R), 0.27 nM (rCB1R)<sup>[1]</sup><i><b>In Vitro:</b></i> Taranabant (MK-0364) binds to human or rat CB1R with an IC<sub>50</sub> of 0.3 and 0.4 nM, respectively, corresponding to a K<sub>i</sub> value of 0.13 and 0.27 nM, respectively. Taranabant binds to the human or rat CB2R with an IC<sub>50</sub> value of 290 and 470 nM, respectively, corresponding to a K<sub>i</sub> value of 170 and 310 nM, respectively. The selectivity ratio of CB1R over CB2R is approximately 1000-fold<sup>[1]</sup>. Taranabant (MK-0364) is a novel, acyclic cannabinoid-1 receptor inverse agonist for the treatment of obesity. IC<sub>50</sub>s of Taranabant for CB1R and CB2R by <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(xì)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/Taranabant.html">www.medchemexpress.cn/Taranabant.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:492.3668<BR>Formula:C20H21Cl2F2N3O3S<BR>SMILES:O=S(C1=CC(C(N2C[C@](CCC3)([H])N3CC2)=O)=C(Cl)C=C1F)(NC4=CC=CC=C4F)=O.Cl<BR>Pathway:Membrane Transporter/Ion Channel; <BR>Mechanisms:Calcium Channel; <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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