GNF2133 是一種有效的、選擇性的、具有口服活性的?DYRK1A?抑制劑，對 DYRK1A 和 GSK3β 的?IC50?分別為 0.0062、>50 μM。GNF2133 對大鼠和人原代 β 細(xì)胞具有良好的增殖能力和功效。GNF2133 顯著提高葡萄糖處理能力并增加胰島素分泌。GNF2133 具有研究1型糖尿病的潛力。

作者：上海偶聯(lián)醫(yī)藥? 生產(chǎn)單位：上海偶聯(lián)醫(yī)藥

生物活性

GNF2133 is a potent, selective and orally active?DYRK1A?inhibitor 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

性狀

Solid

Formula

C24H30N6O2

CAS 號

2561414-56-8

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

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

溶解性數(shù)據(jù)

In Vitro:?

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