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GNF2133

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Catalog No. T40187Cas No. 2561414-56-8

GNF2133 is an effective and selective inhibitor of DYRK1A with IC50s of 6.2 nM. GNF2133 can be used in studies about type 1 diabetes.

GNF2133

GNF2133

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Purity: 98.51%
Catalog No. T40187Cas No. 2561414-56-8
GNF2133 is an effective and selective inhibitor of DYRK1A with IC50s of 6.2 nM. GNF2133 can be used in studies about type 1 diabetes.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$132In StockIn Stock
5 mg$328In StockIn Stock
10 mg$496In StockIn Stock
25 mg$828In StockIn Stock
50 mg$1,230In StockIn Stock
100 mg$1,730-In Stock
1 mL x 10 mM (in DMSO)$376In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:98.51%
Appearance:Solid
Color:Yellow
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Product Introduction

Bioactivity
Description
GNF2133 is an effective and selective inhibitor of DYRK1A with IC50s of 6.2 nM. GNF2133 can be used in studies about type 1 diabetes.
Targets&IC50
DYRK1A:0.0062 μM, GSK-3β:>50 μM
In vitro
GNF2133 has an IC50 of >50 µM for GSK3β. GNF2133 significantly improves glucose disposal capacity and increases insulin secretion[1].
In vivo
In Diphtheria toxin A (RIP-DTA) mice, GNF2133 (3, 10, 30 mg/kg) significantly improves glucose disposal capacity and increased insulin secretion. In CD-1 mice, GNF2133 (30 mg/kg; p.o.) shows moderate plasma exposure and good oral absorption with oral bioavailability of 22.3%[1]. In Wistar Han rat, GNF2133 (30 mg/kg; p.o.) increases in cell proliferation marker Ki67 and insulin and reduces cyclin D1 levels and overall cell density[1].
Chemical Properties
Molecular Weight434.53
FormulaC24H30N6O2
Cas No.2561414-56-8
SmilesCCN1CCN(CC1)C(=O)Nc1cc(ccn1)-c1cn(C2CCOCC2)c2cnccc12
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 4.5 mg/mL (10.36 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.3013 mL11.5067 mL23.0134 mL115.0669 mL
5 mM0.4603 mL2.3013 mL4.6027 mL23.0134 mL
10 mM0.2301 mL1.1507 mL2.3013 mL11.5067 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

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