GSK-3β inhibitor 9 (Compound 9b) is a highly selective, orally bioavailable and potent GSK-3β inhibitor with the IC 50 of 35 nM. GSK-3β inhibitor 9 exhibits good pharmacokinetic profiles including favorable BBB penetration. GSK-3β inhibitor 9 is able to be used for the research of Alzheimer’s disease [1].

GSK-3β inhibitor 9 (Compound 9b) exhibited potent pharmacokinetic properties when administered to GS rats and C57BL/6N mice at doses ranging from 1-3 mg/kg over periods of 1-24 hours. It demonstrated favorable blood-brain barrier (BBB) permeability, indicated by an AUC (area under the curve) 0-24h value of 734 ng•h/g and a brain-to-plasma ratio (Kp value) of 1.6. In experiments utilizing 8-week-old male IGS rats, Compound 9b was administered intravenously and orally at dosages of 1 and 3 mg/kg across various time points (1, 2, 4, 8, 24 hours). This treatment resulted in a volume of distribution (Vdss,iv) ranging from 1134 to 1650 mL/kg, total clearance (CLtotal,iv) between 27.4 and 28.4 mL/min/kg, and a maximum concentration (Cmax,po) from 289.6 to 396.9 ng/mL. Additionally, oral administration led to AUC 0-24 h values between 1229.1 and 1380.6 ng•h/mL, mean residence time (MRTpo) from 2.19 to 3.03 hours, and fraction dosed (Fd%) from 65.5 to 72.8%.