GNF4877
| 中文名称 | GNF4877 |
|---|---|
| 中文同义词 | 化合物GNF4877;(R)-1-(3-(3-氨基-6-(2-氟-5-异丙氧基苯基)吡嗪-2-甲酰胺基)吡啶-4-基)哌啶-3-羧酸 |
| 英文名称 | GNF4877 |
| 英文同义词 | GNF4877;CID 139600315;3-Piperidinecarboxylic acid, 1-[3-[[[3-amino-6-[2-fluoro-5-(1-methylethoxy)phenyl]-2-pyrazinyl]carbonyl]amino]-4-pyridinyl]-, (3R)-;CID 139600315(GNF-4877);GNF 4877,GSK-3,inhibit,Glycogen synthase kinase-3,Glycogen synthase kinase 3,GNF-4877,GNF4877,Inhibitor,Dual specificity tyrosine regulated kinase,Dual specificity tyrosine phosphorylation regulated kinase,DYRK;GNF-4877 GNF4877 |
| CAS号 | 2041073-22-5 |
| 分子式 | C25H27FN6O4 |
| 分子量 | 494.52 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 2041073-22-5.mol |
| 结构式 |  |
GNF4877 性质
| 沸点 | 669.7±55.0 °C(Predicted) |
|---|---|
| 密度 | 1.367±0.06 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | DMSO：4.17 mg/mL（8.43 mM 和升温） |
| 酸度系数(pKa) | 2.82±0.70(Predicted) |
| 形态 | 固体 |
| 颜色 | 浅黄至黄色 |
|
GSK3β 16 nM (IC 50 ) |
DYRK1A 6 nM (IC 50 ) |
High glucose concentrations and glucokinase activators (GKAs) increase Ca 2+ signalling in β-cells, and increase intracellular Ca 2+ leads to activation of calcineurin and nuclear translocation of NFATc proteins. Indeed, concentrations of GNF4877 ((0.1 μM, 0.3 μM) well below the EC 50 for β-cell proliferation are able to induce proliferation in the presence of high glucose or pharmacological activators of glucokinase. Finally, increasing intracellular Ca 2+ with glibenclamide (a sulfonylurea receptor 1 inhibitor) or Bay K8644 (an L-type Ca 2+ channel activator) show additive activity with GNF4877.
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. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/08/19 | HY-129492 | GNF4877 GNF4877 | 2041073-22-5 | 1 mg | 1700元 |
| 2024/08/19 | HY-129492 | GNF4877 GNF4877 | 2041073-22-5 | 5mg | 5300元 |