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GNF4877
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GNF4877图片
CAS NO:2041073-22-5
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
GNF4877是DYRK1AGSK3β的有效抑制剂,IC50值分别为 6 nM 和 16 nM,可导致 NFATc 核输出受阻并增加 β 细胞增殖 (对小鼠 β (R7T1) 细胞的EC50值为 0.66 μM)。
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]

GSK3β

16 nM (IC50)

DYRK1A

6 nM (IC50)

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].

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)[1]
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.
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
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 4.17 mg/mL(8.43 mM;Need ultrasonic and warming)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.0222 mL10.1108 mL20.2216 mL
5 mM0.4044 mL2.0222 mL4.0443 mL
10 mM---------
*

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
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。