中文名称: | GNF4877 | ||||
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英文名称: | GNF4877 | ||||
别名: | GNF4877 (R)-1-(3-(3-Amino-6-(2-fluoro-5-isopropoxyphenyl)pyrazine-2-carboxamido)pyridin-4-yl)piperidine-3-carboxylic acid | ||||
CAS No: | 2041073-22-5 | 分子式: | C25H27FN6O4 | 分子量: | 494.5274 |
CAS No: | 2041073-22-5 | ||||
分子式: | C25H27FN6O4 | ||||
分子量: | 494.5274 |
基本信息
产品编号:G10682 |
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产品名称:GNF4877 |
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CAS: |
2041073-22-5 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
六个月 |
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分子量 |
494.53 |
-20℃ |
一个月 |
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化学名: |
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Solubility (25°C) |
体外 |
DMSO |
32mg/mL (67.51mM) |
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Ethanol |
Insoluble |
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Water |
Insoluble |
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体内(现配现用) |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
2.0222mL |
10.1108mL |
20.2216mL |
5mM |
0.4044mL |
2.0222mL |
4.0443mL |
生物活性
产品描述 |
DYRK1A 和 GSK3β 的有效抑制剂,IC50 值分别为 6nM 和 16nM,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 0.66μM)。 |
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靶点/IC50 |
GSK3β 16nM (IC50) |
DYRK1A 6nM (IC50) |
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体外研究 |
High glucose concentrations and glucokinase activators (GKAs) increase Ca2+signalling in β-cells, and increase intracellular Ca2+ leads to activation of calcineurin and nuclear translocation of NFATc proteins. Indeed, concentrations of GNF4877((0.1M,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. Finally, increasing intracellular Ca2+ with glibenclamide (a sulfonylurea receptor 1 inhibitor) or Bay K8644 (an L-type Ca2+ channel activator) show additive activity with GNF4877. |
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体内研究 |
GNF4877 (50mg/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: |
Double transgenic RIP-DTA male mice (Tg (Ins 2-rtTA) 2 Efr Tg (teto-DTA) 1 Gfi/J) with Doxycycline (28.8±2.4g; 82±2 days) |
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Dosage: |
50mg/kg |
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Administration: |
Oral gavage;twice a day;for 15 days |
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Result: |
Induced β-cell proliferation,increased β-cell mass and insulin content,and improved glycaemic control. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )