产品描述: | A 1070722 is a potent and selective GSK-3 inhibitor, shows high affinity GSK-3α(Ki = 0.6 nM) and GSK-3β(Ki = 0.6 nM). It can penetrate the blood-brain barrier (BBB) and accumulates in brain regions, thus potential for PET radiotracer for the quantification of GSK-3 in brain |
靶点: |
GSK-3α:0.6 nM (ki), GSK-3β:0.6 nM (ki);GSK-3 |
体内研究: |
PET imaging experiments in anesthetized vervet/African green monkey exhibited that A 1070722 penetrated the blood-brain barrier (BBB) and accumulated in brain regions, with highest radioactivity binding in frontal cortex followed by parietal cortex and anterior cingulate, and with the lowest bindings found in caudate, putamen, and thalamus, similarly to the known distribution of GSK-3 in human brain |
参考文献: |
1. Prabhakaran J, et al. Radiosynthesis and in Vivo Evaluation of [11C]A1070722, a High Affinity GSK-3 PET Tracer in Primate Brain. ACS Chem Neurosci. 2017 Aug 16;8(8):1697-1703. |
溶解性: |
Soluble in DMSO |
保存条件: |
2-8°C |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.76 ml |
13.8 ml |
27.601 ml |
5 mM |
0.552 ml |
2.76 ml |
5.52 ml |
10 mM |
0.276 ml |
1.38 ml |
2.76 ml |
50 mM |
0.055 ml |
0.276 ml |
0.552 ml |
|
注意: |
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