GNF4877
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- CAS号:
- 2041073-22-5
- 英文名:
- GNF4877
- 英文别名:
- GNF4877;CID 139600315;GNF-4877 GNF4877;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)-;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
- 中文名:
- GNF4877
- 中文别名:
- 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
- CBNumber:
- CB55540441
- 分子式:
- C25H27FN6O4
- 分子量:
- 494.52
- MOL File:
- 2041073-22-5.mol
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GNF4877化学性质
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沸点:
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669.7±55.0 °C(Predicted)
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密度:
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1.367±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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DMSO: 4.17 mg/mL (8.43 mM and warming)
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酸度系数(pKa):
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2.82±0.70(Predicted)
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GNF4877性质、用途与生产工艺
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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GSK3β
16 nM (IC
50
)
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DYRK1A
6 nM (IC
50
)
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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.
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Animal Model:
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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)
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Dosage:
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50 mg/kg
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Administration:
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Oral gavage; twice a day; for 15 days
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Result:
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Induced β-cell proliferation, increased β-cell mass and insulin content, and improved glycaemic control.
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GNF4877
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-129492 | GNF4877
GNF4877 | 2041073-22-5 | 10mg | 8400元 |
| 2024/01/25 | HY-129492 | GNF4877
GNF4877 | 2041073-22-5 | 1 mg | 1700元 |
2041073-22-5, GNF4877 相关搜索:
- (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
- 化合物GNF4877
- 2041073-22-5
- GNF-4877 GNF4877
- 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
- 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)-
- CID 139600315
- GNF4877