产品
编 号：F741431
分子式：C22H15F2N5O
分子量：403.38
分子式：C22H15F2N5O
分子量：403.38
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规格
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CAS No: 2227279-83-4
产品详情
生物活性：
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.
体内研究：
GSK-3 inhibitor 4 (10 mg/kg, p.o.) 当以 10 mg/kg 的剂量口服纳米悬浮液时，pTau396 减少 37%。GSK-3 inhibitor 4 (2 mg/kg, i.v.; 10 mg/kg, p.o.) 表现出低-中度的清除率，从 15.8 到 23.3 mL/min/kg，以溶液形式口服时吸收良好。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/kg
Administration: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).
体外研究：
GSK-3 inhibitor 4 (compound 40) 对 CDK2 (840-fold, IC50 = 0.47 μM)，CDK5 (1200-fold, IC50 = 0.68 μM)，GSK-3β (IC50 = 0.56 nM)，和 GSK-3α (IC50 = 0.45 nM) 表现出极佳的选择性。GSK-3 inhibitor 4具有良好的渗透性，由于其亲脂性，表现出与血浆蛋白和脑组织结合的高能力。
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.
体内研究：
GSK-3 inhibitor 4 (10 mg/kg, p.o.) 当以 10 mg/kg 的剂量口服纳米悬浮液时，pTau396 减少 37%。GSK-3 inhibitor 4 (2 mg/kg, i.v.; 10 mg/kg, p.o.) 表现出低-中度的清除率，从 15.8 到 23.3 mL/min/kg，以溶液形式口服时吸收良好。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/kg
Administration: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).
体外研究：
GSK-3 inhibitor 4 (compound 40) 对 CDK2 (840-fold, IC50 = 0.47 μM)，CDK5 (1200-fold, IC50 = 0.68 μM)，GSK-3β (IC50 = 0.56 nM)，和 GSK-3α (IC50 = 0.45 nM) 表现出极佳的选择性。GSK-3 inhibitor 4具有良好的渗透性，由于其亲脂性，表现出与血浆蛋白和脑组织结合的高能力。
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