| Identification | Back Directory | [Name]
INDEX NAME NOT YET ASSIGNED | [CAS]
2561414-56-8 | [Synonyms]
β-cell,RIP-DTA mice,Inhibitor,insulin secretion,GNF2133,inhibit,Dual specificity tyrosine regulated kinase,glucose disposal,Dual specificity tyrosine phosphorylation regulated kinase,CD-1 mice,GNF 2133,DYRK,GNF-2133,orally active | [Molecular Formula]
C24H30N6O2 | [MOL File]
2561414-56-8.mol | [Molecular Weight]
434.54 |
| Chemical Properties | Back Directory | [Boiling point ]
712.2±60.0 °C(Predicted) | [density ]
1.33±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [form ]
Solid | [pka]
13.31±0.20(Predicted) | [color ]
Off-white to pink |
| Hazard Information | Back Directory | [Biological Activity]
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]. | [References]
[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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