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A 1070722

A 1070722 是高效的糖原合成酶激酶 3 (GSK-3)选择性抑制剂，与 GSK-3α 和 GSK-3β 结合的Ki 为 0.6 nM。A 1070722 可以穿透血脑屏障并在脑区积聚，具有作为PET 放射性跟踪剂定量测定脑部 GSK-3的潜力。

CAS号

1384424-80-9

分子式

C17H13F3N4O2

主要靶点

GSK-3

仅限科研使用

Cat No : CM20740

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Synonyms

验证数据展示

  • CAS No.: 1384424-80-9

    A 1070722
    CAS#: 1384424-80-9

产品信息

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.

CAS号 1384424-80-9
分子式 C17H13F3N4O2
主要靶点 GSK-3
主要通路 干细胞|PI3K/Akt/mTOR信号通路
分子量 362.31
纯度 99.78%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名

靶点活性

GSK-3β:0.6 nM (ki)|GSK-3α:0.6 nM (ki)

体内活性

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[1].

溶解度

DMSO:83.33 mg/mL (230.00 mM),Sonification is recommended.

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.

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