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货期：电询
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327056-26-8
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电询
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AZD 9272
CAS No. : 327056-26-8
MCE 国际站：AZD 9272
产品活性：AZD 9272 是一种脑渗透性 mGluR5 拮抗剂。
研究领域：GPCR/G Protein | Neuronal Signaling
作用靶点：mGluR
In Vitro: AZD 9272 causes a concentration dependent decrease in the magnitude of the intracellular Ca2+ response to 1.5 μM of the mGluR group I selective agonist DHPG in both the human and the rat mGluR5 expressing cell lines. The maximal inhibition is 100%. The mean IC50 (±SD) value at the human mGluR5 is 7.6±1.1 nM (n=13) for AZD9272. The mean IC50 value at the rat mGluR5 is 2.6±0.3 nM (n=3) for AZD9272. In contrast, 10 μM of AZD9272 does not diminish the response to 10 μM ATP in the background GHEK cells. Increasing concentrations of AZD9272 causes a decrease in the potency and the maximal response of DHPG. AZD9272 completely reverses the glutamate-stimulated (EC80, 80 μM) phosphatidyl inositol hydrolysis in human mGluR5-GHEK cells in a concentration-dependent manner, with IC50 of 26±3 nM (n=21).
In Vivo: The clearance of AZD 9272 is low following a single intravenous dose at 3 μmol/kg and AZD 9272 is eliminated from plasma with terminal half-lives between 2 and 6 h. The terminal half-lives following oral dosing are similar to the half-lives following intravenous dosing. The volume of distribution at steady state is intermediate for AZD9272. AZD9272 causes no cocaine-appropriate responding and causes a non-dose-dependent reduction in response rates at higher doses. AZD9272 at 2.84 mg/kg causes greater than 80% and typically more than 99% MTEP-appropriate responding up to 20 hours after dose, with a decline to approximately 20% at 24 hours after dose, yielding a t1/2 of 21.93 hours, and causes no systematic effects on response rates. The first time point at which AZD9272 causes >90% MTEP-appropriate responding is at 30 minutes after dose.
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文献和实验signaling, #9272, 不能识别磷酸化AKT，只能识别非磷酸化AKT。 所以，最好用磷酸化抗体来做。 liubingood 非磷酸化的多克隆抗体（比如兔多抗）一般是可以识别磷酸化蛋白的，但是通常磷酸化蛋白与非磷酸化蛋白的分子量没有什么区别，所以做出的带子通常是非磷酸化和磷酸化蛋白叠加的带子，而且磷酸化蛋白只占非磷酸化蛋白的很小很小一部分，我们就认为那是由非磷酸化蛋白组成的。要想检测磷酸化蛋白，两种方法：特异的磷酸化抗体检测；采用免疫沉淀的方法先用非磷酸化抗体
！ zhibinx2007 现在比较常用的有两种，可以用AZD235或BEZ8055。 寂寞小美鱼 目前有应用于临床的靶向药物吗？ selleckchem01 可以用于小胶质细胞的有：MK-2206；AT7867；CCT128930； 已经用于临床试验的有MK-2206 现给大家介绍一下主要的AKT抑制剂： MK-2206：a highly selective, potent
为什么你的 qPCR 重复性差？灵敏度低？扩增易受抑制？那是你还不知道数字 PCR
for copy number analysis of the CCL4L genes." Infection, Genetics and Evolution 25 (2014): 28 - 35.4.Oxnard, Geoffrey R., et al. "Association between plasma genotyping and outcomes of treatment with osimertinib (AZD9291) in advanced non–small-cell lung
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