Y-33075是p160 ROCK选择性抑制剂，Ki为140nM。对PKC，cAMP依赖的蛋白激酶和Mypsin轻链激酶抑制性较弱。<BR><a href="https://www.medchemexpress.cn/TAK-438-free-base.html">TAK-438 (free base)</a>产品描述：TAK-438 (free base) is a novel P-CAB (potassium-competitive acid blocker) that reversibly inhibits H+/K+ ATPase with IC50 of 19 nM (pH 6.5), controls gastric acid secretion.
IC50 value: 19 nM [1]
Target: H+/K+ ATPase
in vitro: TAK-438 is a pyrrole derivative with a chemical structure that is completely different from the P-CABs developed to date. TAK-438 inhibits gastric H+/K+ ATPase activity in a concentration-dependent manner. Under neutral conditions (pH 7.5), the inhibitory activity of TAK-438 is almost the same as that under weakly acidic conditions (pH 6.5). TAK-438 does not inhibit Na+/K+ ATPase activity even at concentration 500 times higher than their IC50 values against gastric H+/K+ ATPase activity. TAK-438 inhibits gastric H+/K+ ATPase in a K+ competitive manner with Ki of 3 nM [2].
in vivo: TAK-438 inhibits basal gastric acid secretion in a dose-dependent manner, and the ID50 value is 1.26 mg/kg. Intravenous administration of TAK-438 dose-dependently increases the pH<br><br>
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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/TAK-438-free-base.html">www.medchemexpress.cn/TAK-438-free-base.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:280.3244<BR>Formula:C16H16N4O<BR>SMILES:O=C(NC1=C2C(NC=C2)=NC=C1)C3=CC=C(C=C3)[C@H](N)C<BR>Pathway:Cell Cycle/DNA Damage; Stem Cell/Wnt; TGF-beta/Smad; <BR>Mechanisms:ROCK; <BR>Research Area:Cardiovascular 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
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