GNF4877
作者：齐岳
发布时间：2023-09-13
16:59:54
点击数：
产品名称：GNF4877
产品描述：
| 产品描述 | GNF4877 is a potent DYRK1A and GSK3β inhibitor (IC50s: 6 nM and 16 nM). It leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation cells. |
| 靶点活性 | GSK3β:16 nM, DYRK1A:6 nM |
| 体外活性 | Concentrations of GNF4877 (0.1?μM, 0.3?μM) well below the EC50 for β-cell proliferation are able to induce proliferation in the presence of high glucose or pharmacological activators of glucokinase. High glucose concentrations and glucokinase activators (GKAs) increase Ca2+ signaling in β-cells, and increase intracellular Ca2+ leads to activation of calcineurin and nuclear translocation of NFATc proteins.?Finally, increasing intracellular Ca2+ with glibenclamide or Bay K8644 shows additive activity with GNF4877. |
| 体内活性 | In double transgenic RIP-DTA male mice, GNF4877 (50 mg/kg; oral gavage; twice a day; for 15 days) treatment induces β-cell proliferation, increases β-cell mass and insulin content, and improves glycaemic control. |
| 分子量 | 494.52 |
| 分子式 | C25H27FN6O4 |
| CAS No. | 2041073-22-5 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 4.17 mg/mL (8.43 mM),Need ultrasonic and warming
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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