GNF4877
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 |
| InChIKey | UZIATSFXNVOVFE-OAHLLOKOSA-N |
| SMILES | N1(C2C=CN=CC=2NC(C2=NC(C3=CC(OC(C)C)=CC=C3F)=CN=C2N)=O)CCC[C@@H](C(O)=O)C1 |
GNF4877 用途与合成方法
|
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. |
GNF4877 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2026-09-15 | HY-129492 | GNF4877 | 2041073-22-5 | 1 mg | 990 |
| 2026-09-15 | HY-129492 | GNF4877 | 2041073-22-5 | 5mg | 3500 |
