产品
编 号：F251167
分子式：C25H27FN6O4
分子量：494.52
分子式：C25H27FN6O4
分子量：494.52
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 2041073-22-5
产品详情
生物活性：
GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC50s of 6?nM and 16?nM, respectively, which leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation (EC50 of 0.66?μM for mouse β (R7T1) cells).
体内研究：
GNF4877 (50 mg/kg; oral gavage; twice a day; for 15 days; double transgenic RIP-DTA male mice) treatment induces β-cell proliferation, increases β-cell mass and insulin content, and improves glycaemic control.Animal Model:Double transgenic RIP-DTA male mice (Tg (Ins 2-rtTA) 2 Efr Tg (teto-DTA) 1 Gfi/J) with Doxycycline (28.8±2.4?g; 82±2 days)
Dosage:50 mg/kg
Administration:Oral gavage; twice a day; for 15 days
Result:Induced β-cell proliferation, increased β-cell mass and insulin content, and improved glycaemic control.
体外研究：
High glucose concentrations and glucokinase activators (GKAs) increase Ca2+ signalling in β-cells, and increase intracellular Ca2+ leads to activation of calcineurin and nuclear translocation of NFATc proteins. Indeed, concentrations of GNF4877 ((0.1?μM, 0.3?μM) well below the EC50 for β-cell proliferation are able to induce proliferation in the presence of high glucose or pharmacological activators of glucokinase. Finally, increasing intracellular Ca2+ with glibenclamide (a sulfonylurea receptor 1 inhibitor) or Bay K8644 (an L-type Ca2+ channel activator) show additive activity with GNF4877.
GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC50s of 6?nM and 16?nM, respectively, which leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation (EC50 of 0.66?μM for mouse β (R7T1) cells).
体内研究：
GNF4877 (50 mg/kg; oral gavage; twice a day; for 15 days; double transgenic RIP-DTA male mice) treatment induces β-cell proliferation, increases β-cell mass and insulin content, and improves glycaemic control.Animal Model:Double transgenic RIP-DTA male mice (Tg (Ins 2-rtTA) 2 Efr Tg (teto-DTA) 1 Gfi/J) with Doxycycline (28.8±2.4?g; 82±2 days)
Dosage:50 mg/kg
Administration:Oral gavage; twice a day; for 15 days
Result:Induced β-cell proliferation, increased β-cell mass and insulin content, and improved glycaemic control.
体外研究：
High glucose concentrations and glucokinase activators (GKAs) increase Ca2+ signalling in β-cells, and increase intracellular Ca2+ leads to activation of calcineurin and nuclear translocation of NFATc proteins. Indeed, concentrations of GNF4877 ((0.1?μM, 0.3?μM) well below the EC50 for β-cell proliferation are able to induce proliferation in the presence of high glucose or pharmacological activators of glucokinase. Finally, increasing intracellular Ca2+ with glibenclamide (a sulfonylurea receptor 1 inhibitor) or Bay K8644 (an L-type Ca2+ channel activator) show additive activity with GNF4877.
产品资料
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