| CAS NO: | 2561414-56-8 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| Cas No. | 2561414-56-8 |
| 分子式 | C24H30N6O2 |
| 分子量 | 434.53 |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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 1 diabetes[1]. GNF2133 (30 mg/kg; p.o.) shows good oral absorption with oral bioavailability of 22.3%[1].GNF2133 (30 mg/kg; p.o.; once a day for 5 days) shows the ability to proliferate β-cells in vivo[1].GNF2133 (3, 10, 30 mg/kg) significantly improves glucose disposal capacity and increased insulin secretion in RIP-DTA mice[1].Pharmacokinetic Parameters of GNF2133 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 (%)22.3CD-1 mice; 30 mg/kg; 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. |
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