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JNJ16259685

发布日期：2017-10-26   浏览次数：0
核心提示：a href=https://www.medchemexpress.com/JNJ16259685.htmlJNJ16259685/a产品描述：JNJ16259685 is a selective antagonist of bm
<a href="https://www.medchemexpress.com/JNJ16259685.html">JNJ16259685</a>产品描述：JNJ16259685 is a selective antagonist of <b>mGlu1 receptor</b>, and inhibits the synaptic activation of mGlu1 in a concentration-dependent manner with <b>IC<sub>50</sub></b> of 19 nM.

IC50 & Target: IC50: 19 nM (mGlu1)

<i><b>In Vitro:</b></i> JNJ16259685 potently and completely inhibits the glutamate (30 μM)-induced increase in intracellular Ca<sup>2+</sup> concentrations at the rat mGlu1a receptor with an IC<sub>50</sub> value of 3.24±1.00 nM. IC<sub>50</sub> values for CPCCOEt and BAY 36-7620 are 17.8±10.3 μM and 161±38 nM, respectively. The potency of JNJ16259685 in blocking glutamate (30 μM)-induced Ca<sup>2+</sup> mobilization at the human mGlu1a receptor is 1.21±0.53 nM (IC<sub>50</sub> n=3). JNJ16259685 inhibits the glutamate (3 μM)-induced rise in intracellular Ca<sup>2+</sup> concentrations at the rat mGlu5a receptor with an IC<sub>50</sub> value of 1.31±0.39 μM (n=4). JNJ16259685 blocks glutamate (3 μM)-induced Ca<sup>2+</sup> mobilization at the human mGlu5 receptor with <br><br>
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<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>
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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/jnj16259685.html">www.medchemexpress.cn/jnj16259685.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="">
 
 
 
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