Description |
The racemic mixture of a cell-permeable oxadiazolo-benzofuranylphenylsulfoxide that inhibits GSK-3β (IC 50 = 35, 34, and 140 nM using the racemate, the ( S ), and the ( R ) enantiomer, respectively) in a highly selective manner as evidenced by its eutomer's inability to inhibit 10 other serine/threonine and 12 other tyrosine kinases even at concentrations as high as 10 µM. Reported to exhibit good aqueous solubility (38 µg racemate/ml pH 6.8 buffer) and pharmacokinetic properties, being orally active in both rats and mice in vivo (Plasma AUC 0-24h = 1380.6 and 457 ng•h/mL, respectively; 3 mg eutomer/kg via p.o.)
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