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AZ PFKFB3 26

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Catalog No. T14365Cas No. 1704740-52-2

AZ PFKFB3 26 is an effective and selective PFKFB3 inhibitor with an IC50 of 23 nM. The IC50s for PFKFB1 and PFKFB2 are 2.06 and 0.384 μM, respectively.

AZ PFKFB3 26

AZ PFKFB3 26

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Purity: 99.85%
Catalog No. T14365Cas No. 1704740-52-2
AZ PFKFB3 26 is an effective and selective PFKFB3 inhibitor with an IC50 of 23 nM. The IC50s for PFKFB1 and PFKFB2 are 2.06 and 0.384 μM, respectively.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
2 mg$30In StockIn Stock
5 mg$43In StockIn Stock
10 mg$76In StockIn Stock
25 mg$173In StockIn Stock
50 mg$298In StockIn Stock
100 mg$415-In Stock
1 mL x 10 mM (in DMSO)$54In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
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:99.85%
Appearance:Solid
Color:White
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Product Introduction

AZ PFKFB3 26 AI Summary
AZ PFKFB3 26 is a bioactive compound exhibiting potent inhibitory activity against recombinant human PFKFB1, PFKFB2, and PFKFB3 enzymes, with varying IC50 values. It has moderate lipophilicity, reflected by a logD value of 3.5, and good aqueous solubility. The compound shows a low fraction unbound in rat plasma and a moderate fraction unbound in human plasma. In cellular assays, AZ PFKFB3 26 inhibits PFKFB3, reducing fructose-1,6-bisphosphate formation and lactate secretion. It demonstrates good permeability in human Caco-2 cells and possesses an efflux ratio. The compound has favorable oral bioavailability in both CD1 mouse and Wistar rat models, with good absorption and a relatively low volume of distribution in mice compared to rats. It undergoes species-dependent clearance rates. In vivo, the compound exhibits a reasonable half-life in mice and rats and achieves high exposure levels in nude mice based on AUC and Cmax values. Additionally, AZ PFKFB3 26 shows selectivity towards PFKFB2 over PFKFB3 based on IC50 values..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
AZ PFKFB3 26 is an effective and selective PFKFB3 inhibitor with an IC50 of 23 nM. The IC50s for PFKFB1 and PFKFB2 are 2.06 and 0.384 μM, respectively.
Targets&IC50
PFKFB1:2.06 μM, PFKFB3:23 nM, PFKFB2:0.384 μM
Chemical Properties
Molecular Weight402.49
FormulaC24H26N4O2
Cas No.1704740-52-2
SmilesCC(C)Cn1cc(C#N)c2cc(Oc3ccc(NC(=O)[C@@H]4CCCN4)cc3)ccc12
Relative Density.1.24 g/cm3 (Predicted)
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 (11.18 mM), when pH is adjusted to 3 with HCl. Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.4845 mL12.4227 mL24.8453 mL124.2267 mL
5 mM0.4969 mL2.4845 mL4.9691 mL24.8453 mL
10 mM0.2485 mL1.2423 mL2.4845 mL12.4227 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

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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

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