GNF2133 hydrochloride 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 ?M。GNF2133 hydrochloride 对大鼠和人原代 β 细胞具有良好的增殖能力和功效。GNF2133 hydrochloride 显著提高葡萄糖处理能力并增加胰岛素分泌。GNF2133 hydrochloride 具有研究1型糖尿病的潜力。
货号:ajcx38176
CAS:2561414-57-9
分子式:C24H31ClN6O2
分子量：470.99
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

GNF2133 hydrochloride is a potent, selective and orally active DYRK1A inhibitor with IC50s of 0.0062, >50 &#181M for DYRK1A and GSK3β, respectively. GNF2133 hydrochloride shows good proliferation potency and efficacy on rat and human primary β-cell. GNF2133 hydrochloride significantly improves glucose disposal capacity and increases insulin secretion. GNF2133 hydrochloride has the potential for the research of type 1 diabetes[1].

GNF2133 hydrochloride (30 mg/kg; p.o.) shows good oral absorption with oral bioavailability of 22.3%[1].GNF2133 hydrochloride (30 mg/kg; p.o.; once a day for 5 days) shows the ability to proliferate β-cells in vivo[1].GNF2133 hydrochloride (3, 10, 30 mg/kg) significantly improves glucose disposal capacity and increased insulin secretion in RIP-DTA mice[1].Pharmacokinetic Parameters of GNF2133 hydrochloride in CD-1 mice[1].                plasma (iv)       plasma (po)       pancreas (po) CL (mL/min/kg)23.5Vss (L/kg)11AUC (h.nM)326810974144420 Cmax(nM)1977167513319tmax<(h)0.033.03.0Clast(nM)36.6191324t1/2<(h)6.63.46.6f 30="" 22.3cd-1="" p.o.sup="">[1].

[1]. Liu YA, et al. Selective DYRK1A Inhibitor for the Treatment of Type 1 Diabetes: Discovery of 6-Azaindole Derivative GNF2133. J Med Chem. 2020 Mar 26;63(6):2958-2973.