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A 1070722 is a potent and selective GSK-3 inhibitor, exhibiting high affinity for both GSK-3α (Ki = 0.6 nM) and GSK-3β (Ki = 0.6 nM). It can penetrate the blood-brain barrier (BBB) and accumulate in brain regions, indicating potential use as a PET radiotracer for quantifying GSK-3 in the brain.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $38 | In Stock | |
10 mg | $58 | In Stock | |
25 mg | $118 | In Stock | |
50 mg | $213 | In Stock | |
100 mg | $320 | In Stock | |
1 mL x 10 mM (in DMSO) | $39 | In Stock |
Description | A 1070722 is a potent and selective GSK-3 inhibitor, exhibiting high affinity for both GSK-3α (Ki = 0.6 nM) and GSK-3β (Ki = 0.6 nM). It can penetrate the blood-brain barrier (BBB) and accumulate in brain regions, indicating potential use as a PET radiotracer for quantifying GSK-3 in the brain. |
Targets&IC50 | GSK-3β:0.6 nM (ki), GSK-3α:0.6 nM (ki) |
In vivo | 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]. |
Molecular Weight | 362.31 |
Formula | C17H13F3N4O2 |
Cas No. | 1384424-80-9 |
Smiles | COc1ccc2c(NC(=O)Nc3cccc(n3)C(F)(F)F)ccnc2c1 |
Relative Density. | 1.461 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 83.33 mg/mL (230.00 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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