产品
编 号：F741432
分子式：C23H15FN6O
分子量：410.4
分子式：C23H15FN6O
分子量：410.4
产品类型
规格
价格
是否有货
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
结构图
CAS No: 2227279-84-5
产品详情
生物活性：
GSK-3 inhibitor 3 is a selective, orally active and brain-penetrant inhibitor of GSK-3, with IC50s of 0.35 nM and 0.25 nM for GSK-3α and GSK-3β, respectively. GSK-3 inhibitor 3 lowers levels of tau protein phosphorylation at S396 in a triple-transgenic mouse Alzheimer’s disease model, with IC50 of 10 nM. GSK-3 inhibitor 3 can be used for neurological disease research.
体内研究：
GSK-3 inhibitor 3 (Compound 34) (静脉注射 2 mg/kg，口服 10 mg/kg) 显示在雄性 C57BL6 小鼠中 T1/2 为 2.5 小时（静脉注射），口服生物利用度 (F%) 约 100%。GSK-3 inhibitor 3 (10 mg/kg，单次口服)使三重转基因小鼠阿尔茨海默病模型中Tau 396 位磷酸化水平降低 33%。Pharmacokinetic parameters for GSK-3 inhibitor 3(Compound 34) in MiceRouteDose (mg/kg) CL (mL?min-1/kg-1)Vss (L/kg)>Tmax (h) MRT (h) T1/2 (h) AUCtot (μM/h)Cmax (μM)F (%)
i.v.223.35.43.92.5///
p.o.10////24.33.5~100
Animal Model:Alzheimer’s disease model using LaFerla 3xTg-C57BL6 mice
Dosage:10 mg/kg
Administration:Oral gavage (p.o.)
Result:Produced a 37% reduction in pTau396.
体外研究：
GSK-3 inhibitor 3 (Compound 34) (1 μM) 是 CDK2 和 CDK5 的高选择性抑制剂，对 CDK2 和 CDK5 的 IC50 分别为 0.22 μM 和 1.3 μM 。
GSK-3 inhibitor 3 is a selective, orally active and brain-penetrant inhibitor of GSK-3, with IC50s of 0.35 nM and 0.25 nM for GSK-3α and GSK-3β, respectively. GSK-3 inhibitor 3 lowers levels of tau protein phosphorylation at S396 in a triple-transgenic mouse Alzheimer’s disease model, with IC50 of 10 nM. GSK-3 inhibitor 3 can be used for neurological disease research.
体内研究：
GSK-3 inhibitor 3 (Compound 34) (静脉注射 2 mg/kg，口服 10 mg/kg) 显示在雄性 C57BL6 小鼠中 T1/2 为 2.5 小时（静脉注射），口服生物利用度 (F%) 约 100%。GSK-3 inhibitor 3 (10 mg/kg，单次口服)使三重转基因小鼠阿尔茨海默病模型中Tau 396 位磷酸化水平降低 33%。Pharmacokinetic parameters for GSK-3 inhibitor 3(Compound 34) in MiceRouteDose (mg/kg) CL (mL?min-1/kg-1)Vss (L/kg)>Tmax (h) MRT (h) T1/2 (h) AUCtot (μM/h)Cmax (μM)F (%)
i.v.223.35.43.92.5///
p.o.10////24.33.5~100
Animal Model:Alzheimer’s disease model using LaFerla 3xTg-C57BL6 mice
Dosage:10 mg/kg
Administration:Oral gavage (p.o.)
Result:Produced a 37% reduction in pTau396.
体外研究：
GSK-3 inhibitor 3 (Compound 34) (1 μM) 是 CDK2 和 CDK5 的高选择性抑制剂，对 CDK2 和 CDK5 的 IC50 分别为 0.22 μM 和 1.3 μM 。
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