GSK-3 inhibitor 4

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

GSK-3 inhibitor 4 是一种具有口服活性和脑渗透性的 GSK-3，CDK2 和 CDK5的抑制剂，IC50 值分别为 0.56 nM (GSK-3β)，0.45 nM (GSK-3α)，0.47 μM，0.68 μM。GSK-3 inhibitor 4 能有效降低 Tau protein 水平。GSK-3 inhibitor 4 可用于阿尔茨海默症的研究 (AD)。

GSK-3 inhibitor 4 is an orally active and brain-penetrant inhibitor of GSK-3, CDK2, and CDK5, with IC50 values of 0.56 nM (GSK-3β), 0.45 nM (GSK-3α), 0.47 μM, and 0.68 μM, respectively. GSK-3 inhibitor 4 effectively reduces the phosphorylation level of Tau protein. GSK-3 inhibitor 4 can be used in Alzheimer's disease (AD) studies.

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Animal Model:3xTg mice were bred onto the C57BL6 background and bred as homozygotes. Male animals between the ages of five to seven months were used for the study.Dosage:10 mg/kgAdministration:Oral gavage (p.o.) Result:Produced a 37% reduction in pTau396, when administered orally as a nanosuspension at a dose of 10 mg/kg.Animal Model:male C57BL6 mice (Pharmacokinetic assay)Dosage:2 mg/kg, 10 mg/kg. Administration: Kept for 8 h fasting prior to formulation administration. intravenous and oral routes of administration to mice at a dose of 2 and 10 mg/kg, respectively.Result:Exhibited clearance ranging from 15.8 to 23.3 mL /min/kg , halflives ranging from 2.5 to 2.9 h and were readily orally bioavailable (F% = 53).

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PI3K/Akt/mTOR signaling

GSK-3

GSK-3 | CDK

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2227279-83-4

403.38

C22H15F2N5O

>98% (HPLC)

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N(C(=O)C1=NC(NC2=CC=C(F)C=C2)=NC=C1)C=3C(=CC=NC3)C4=CC=C(F)C=C4

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(-20℃)

With Ice Pack

≥ 2 years