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描述 | GNF2133 is a potent, selective, and orally bioavailable DYRK1A inhibitor with an IC50 of 0.0062 μM for DYRK1A and over 50 μM for GSK3β. It displays strong proliferative effectiveness on rat and human primary β-cells, significantly enhances glucose disposal, and boosts insulin secretion. GNF2133 holds potential for research into type 1 diabetes[1]. |
体内研究 | GNF2133, administered orally at a dose of 30 mg/kg, demonstrates favorable oral absorption with a bioavailability of 22.3%[1]. NF2133, given orally at 30 mg/kg daily for five days, has shown the capacity to promote β-cell proliferation in vivo[1]. NF2133 at doses of 3, 10, and 30 mg/kg markedly enhances glucose disposal and boosts insulin secretion in RIP-DTA mice[1]. Pharmacokinetic Profile of GNF2133 in CD-1 Mice[1]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.30mL 0.46mL 0.23mL |
11.51mL 2.30mL 1.15mL |
23.01mL 4.60mL 2.30mL |
CAS号 | 2561414-56-8 |
分子式 | C24H30N6O2 |
分子量 | 434.53 |
别名 | |
运输 | 蓝冰 |
存储条件 |
粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 3 mg/mL(6.9 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |