GNF2133 hydrochloride is a potent, selective and orally active DYRK1A inhibitor with IC 50 s of 0.0062, >50 µM 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 In Vivo GNF2133 hydrochloride (30 mg/kg; p.o.) shows good oral absorption with oral bioavailability of 22.3% . GNF2133 hydrochloride (30 mg/kg; p.o.; once a day for 5 days) shows the ability to proliferate β-cells in vivo . GNF2133 hydrochloride (3, 10, 30 mg/kg) significantly improves glucose disposal capacity and increased insulin secretion in RIP-DTA mice . Pharmacokinetic Parameters of GNF2133 hydrochloride in CD-1 mice . plasma (iv) plasma (po) pancreas (po) CL (mL/min/kg) 23.5 / / V ss (L/kg) 11 / / AUC (h·nM) 3268 10974 144420 C max (nM) 1977 1675 13319 t max IC50& Target:DYRK1A 0.0062 μM (IC 50 ) GSK3β >50 μM (IC 50 )
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GNF2133 hydrochloride
CAS number：2561414-57-9 molecular formula：C24H31ClN6O2
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| Chinese alias | GNF2133盐酸盐 | ||
| English alias | - | ||
| CAS number | 2561414-57-9 | molecular formula | C24H31ClN6O2 |
| molecular weight | 470.99 g/mol | Exact mass | - |
| PSA | - | logp | - |
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