GNF4877
- CAS号:2041073-22-5
- 英文名:GNF4877
- 中文名:GNF4877
- CBNumber:CB55540441
- 分子式:C25H27FN6O4
- 分子量:494.52
- MOL File:2041073-22-5.mol
- 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 and warming)
- 酸度系数(pKa) :2.82±0.70(Predicted)
GNF4877性质、用途与生产工艺
- 生物活性 GNF4877是 DYRK1A 和 GSK3β 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)。
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靶点
GSK3β
16 nM (IC 50 )
DYRK1A
6 nM (IC 50 )
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体外研究
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.
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体内研究
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.
- 更新日期:2024/04/30
- 产品编号:HY-129492
- 产品名称:GNF4877 GNF4877
- CAS编号:2041073-22-5
- 包装:10mg
- 价格:8400元
- 更新日期:2024/01/25
- 产品编号:HY-129492
- 产品名称:GNF4877 GNF4877
- CAS编号:2041073-22-5
- 包装:1 mg
- 价格:1700元
- 公司名称:TargetMol Chemicals Inc.
- 联系电话:+1-781-999-5354 +1-00000000000
- 电子邮件:marketing@targetmol.com
- 国家:美国
- 产品数:19892
- 优势度:58
- 公司名称:MedChemExpress
- 联系电话:--
- 电子邮件:sales@medchemexpress.com
- 国家:美国
- 产品数:6398
- 优势度:58