GSK-3β inhibitor 13 

GSK-3β inhibitor 13 (compound 47) is an orally active and potent GSK-3β inhibitor with blood-brain permeability. GSK-3β inhibitor 13 inhibits GSK-3β and GSK-3α with IC₅₀s of 0.73 nM and 0.35 nM, respectively. GSK-3β inhibitor 13 significantly decreases the phosphorylation of tau (IC₅₀=58 nM), which leads the formation of the neurofibrillary tangles associated with Alzheimer's disease^[1].

GSK-3β inhibitor 13 has an exposure of 3.8 μM in plasma and 1.3 μM in brain, resulting in a brain-to-plasma (B/P) ratio of 0.34^[1].
GSK-3β inhibitor 13 (30 mg/kg; p.o.; single dose) results in a 52% reduction in pTau396 in in LaFerla 3xTg-C57BL6 mice^[1].

Pharmacokinetic Analysis in Mice^[1]

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

414.46

C₂₃H₂₂N₆O₂

2227316-74-5

O=C(C1=CC=NN2C1=NC(C3=CC=CC=C3)=C2)NC4=C(C=CN=C4)N5CCOC(C5)C

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Hartz RA, et al. Design, Structure-Activity Relationships, and In Vivo Evaluation of Potent and Brain-Penetrant Imidazo[1,2-b]pyridazines as Glycogen Synthase Kinase-3β (GSK-3β) Inhibitors. J Med Chem. 2023 Mar 23;66(6):4231-4252.  [Content Brief]