GNF2133 是一种有效的、选择性的、具有口服活性的 DYRK1A抑制剂，对 DYRK1A 和 GSK3β 的 IC50分别为 0.0062、>50 µM。GNF2133 对大鼠和人原代 β 细胞具有良好的增殖能力和功效。GNF2133 显著提高葡萄糖处理能力并增加胰岛素分泌。GNF2133 具有研究1型糖尿病的潜力。

作者：上海偶联医药  生产单位：上海偶联医药

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生物活性

GNF2133 is a potent, selective and orally active DYRK1Ainhibitor with IC50s of 0.0062, >50 µM for DYRK1A and GSK3β, respectively. GNF2133 shows good proliferation potency and efficacy on rat and human primary β-cell. GNF2133 significantly improves glucose disposal capacity and increases insulin secretion. GNF2133 has the potential for the research of type 

分子量

434.53

性状

Solid

Formula

C24H30N6O2

CAS 号

2561414-56-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder-20°C3 years4°C2 yearsIn solvent-80°C6 months-20°C1 month

溶解性数据

In Vitro: 

DMSO : 4 mg/mL(9.21 mM;ultrasonic and warming and heat to 60°C)