CAS NO: | 2041073-22-5 |
包装 | 价格(元) |
1mg | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
生物活性 | GNF4877 is a potentDYRK1AandGSK3βinhibitor withIC50s 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 (EC50of 0.66 μM for mouse β (R7T1) cells)[1]. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | 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 theEC50for 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[1]. | ||||||||||||||||
体内研究 (In Vivo) | 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[1].
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分子量 | 494.52 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C25H27FN6O4 | ||||||||||||||||
CAS 号 | 2041073-22-5 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 4.17 mg/mL(8.43 mM;Need ultrasonic and warming) 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |