2041073-22-5
2041073-22-5 结构式
基本信息
CID 139600315
CID 139600315(GNF-4877)
3-Piperidinecarboxylic acid, 1-[3-[[[3-amino-6-[2-fluoro-5-(1-methylethoxy)phenyl]-2-pyrazinyl]carbonyl]amino]-4-pyridinyl]-, (3R)-
物理化学性质
| 报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
| 2025/05/22 | HY-129492 | GNF4877 GNF4877 | 2041073-22-5 | 1 mg | 990元 |
| 2025/05/22 | HY-129492 | GNF4877 GNF4877 | 2041073-22-5 | 5mg | 3500元 |
| 2025/05/22 | HY-129492 | GNF4877 GNF4877 | 2041073-22-5 | 10mg | 5600元 |
常见问题列表
|
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. |