[CAS NO. 2561414-56-8] GNF2133
PRODUCTS SPECIFICATIONS [2561414-56-8]
DESCRIPTION [2561414-56-8]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 434.53 |
| Molecular Formula | C24H30N6O2 |
| SMILES | CCN1CCN(CC1)C(NC2=NC=CC(C3=CN(C4=CN=CC=C34)C5CCOCC5)=C2)=O |
Summary
GNF2133 is a potent, selective and orally active DYRK1A inhibitor with IC 50 s 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] .
IC50 & Target
|
DYRK1A 0.0062 μM (IC 50 ) |
GSK3β >50 μM (IC 50 ) |
In Vivo
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) | 23.5 | / | / |
| V ss (L/kg) | 11 | / | / |
| AUC (h·nM) | 3268 | 10974 | 144420 |
| C max (nM) | 1977 | 1675 | 13319 |
| t max <(h) | 0.03 | 3.0 | 3.0 |
| C last (nM) | 36.6 | 19 | 1324 |
| t 1/2 <(h) | 6.6 | 3.4 | 6.6 |
| F (%) | / | 22.3 | / |
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | CD-1 mice [1] |
| Dosage: | 30 mg/kg |
| Administration: | P.o. |
| Result: | Showed good oral absorption and moderate plasma exposure with oral bioavailability of 22.3%. |
| Animal Model: | Wistar Han rat [1] |
| Dosage: | 30 mg/kg (0.5% methylcellulose + Tween-80) |
| Administration: | P.o.; once a day for 5 days |
| Result: | Increased cyclin D1 levels and overall cell density, and increased in cell proliferation marker Ki67 and insulin. |
| Animal Model: | Diphtheria toxin A (RIP-DTA) mice [1] |
| Dosage: | 3, 10, 30 mg/kg (20 mg/kg doxycycline (Dox) for 5 days) |
| Administration: | P.o., once a day for 35 days |
| Result: | Significantly improves glucose disposal capacity and increased insulin secretion. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 4 mg/mL ( 9.21 mM ; ultrasonic and warming and heat to 60°C)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.3013 mL | 11.5067 mL | 23.0134 mL |
| 5 mM | 0.4603 mL | 2.3013 mL | 4.6027 mL |
| 10 mM | --- | --- | --- |