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。

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.

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].

1384424-80-9

C17H13F3N4O2

362.31

DMSO:83.33 mg/mL (230.00 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years