GSK-3β inhibitor 13_product_DataBase

Bioactivity	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].
In Vivo	GSK-3β inhibitor 13 在血浆中的暴露量为 3.8 μM，在脑中的暴露量为 1.3 μM，导致脑-血浆 (B/P) 比率为 0.34[1]。GSK-3β inhibitor 13 (30 mg/kg；口服；单剂量) 在 LaFerla 3xTg-C57BL6 小鼠中降低 52% 的 pTau396 水平[1]。在小鼠中的药代动力学分析[1]Route
Name	GSK-3β inhibitor 13
CAS	2227316-74-5
Formula	C23H22N6O2
Molar Mass	414.46
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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.

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