INDEX NAME NOT YET ASSIGNED manufacturers
- GNF2133
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- $132.00 / 1mg
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2024-10-28
- CAS:2561414-56-8
- Min. Order:
- Purity: 98.11%
- Supply Ability: 10g
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| | INDEX NAME NOT YET ASSIGNED Basic information |
| Product Name: | INDEX NAME NOT YET ASSIGNED | | 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;4-Ethyl-N-(4-(1-(tetrahydro-2H-pyran-4-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl)pyridin-2-yl)piperazine-1-carboxamide;4-ethyl-N-{4-[1-(oxan-4-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]pyridin-2-yl}piperazine-1-carboxamide | | CAS: | 2561414-56-8 | | MF: | C24H30N6O2 | | MW: | 434.54 | | EINECS: | | | Product Categories: | | | Mol File: | 2561414-56-8.mol |  |
| | INDEX NAME NOT YET ASSIGNED Chemical Properties |
| 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 |
| | INDEX NAME NOT YET ASSIGNED Usage And Synthesis |
| 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. |
| | INDEX NAME NOT YET ASSIGNED Preparation Products And Raw materials |
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