Shopping Cart

Your shopping cart is currently empty

PFK-158

Name: PFK-158
Brand: TargetMol
SKU: T3105
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

Copy Product Info

🥰Excellent

Catalog No. T3105Cas No. 1462249-75-7

PFK-158 is an effective and specific inhibitor PFKFB3.

PFK-158

Copy Product Info

🥰Excellent

Purity: 99.16%

Catalog No. T3105Cas No. 1462249-75-7

PFK-158 is an effective and specific inhibitor PFKFB3.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$30	In Stock	In Stock
2 mg	$40	In Stock	In Stock
5 mg	$64	In Stock	In Stock
10 mg	$97	In Stock	In Stock
25 mg	$183	In Stock	In Stock
50 mg	$287	In Stock	In Stock
100 mg	$455	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$70	In Stock	In Stock

Add to Cart

Add to Quotation

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.

Questions

Batch Information

Select Batch

Purity:99.16%

Color:White to Yellow

Resource Download

COA LCMS

Product Introduction

PFK-158 AI Summary

PFK-158 demonstrates diverse bioactivities, including antiviral, antibacterial, enzymatic inhibition, and pharmacokinetic properties. Notably, it exhibits antiviral activity against SARS-CoV-2, with an inhibition rate of 1.89% in Caco-2 cells at 10 µM concentration after 48 hours and -0.1% inhibition in VERO-6 cells under similar conditions, as determined through high content imaging. It also inhibits the SARS-CoV-2 3CL-Pro protease by 18.31% at 20 µM, as measured by a FRET-based assay. The compound shows significant antibacterial activity against various strains, including methicillin-sensitive and resistant Staphylococcus, vancomycin-sensitive and resistant Enterococcus species, and ESBL-positive and negative Escherichia coli. It is particularly more effective against methicillin-sensitive strains and exhibits synergistic activity with colistin against carbapenem-resistant E. coli and Enterobacter cloacae isolates. The cytotoxicity against A549 cells is moderate, with an IC50 value of 15000.0 nM. PFK-158 also functions as an inhibitor of the human HDAC6 enzyme, with 36.79% inhibition using a commercial peptide substrate and -2.03% with a custom peptide substrate. Additionally, it inhibits PFKFB3 in unknown origin cells and Jurkat cells with IC50 values of 137.0 nM and 1600.0 nM, respectively. Metabolically, it has a stability of 37.0% in human liver microsomes and a half-life of 10.5 hours in BALB/c mice, with an AUC of 3235.0 ng.hr.mL-1 and a clearance rate of 26.0 mL.min-1.kg-1 at an intravenous dose of 5 mg/kg. The maximum tolerated dose (MTD) toxicity assessment in Sprague-Dawley rats exceeds 40.0 mg/kg..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	PFK-158 is an effective and specific inhibitor PFKFB3.
Targets&IC50	PFKFB3:137 nM (IC50 )

Chemical Properties

Molecular Weight	328.29
Formula	C₁₈H₁₁F₃N₂O
Cas No.	1462249-75-7
Smiles	FC(F)(F)c1ccc2ccc(\C=C\C(=O)c3ccncc3)nc2c1
Relative Density.	1.346 g/cm3 (Predicted)

Storage & Solubility Information

Storage

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 13.16 mg/mL (40.09 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.0461 mL	15.2304 mL	30.4609 mL	152.3044 mL
5 mM	0.6092 mL	3.0461 mL	6.0922 mL	30.4609 mL
10 mM	0.3046 mL	1.5230 mL	3.0461 mL	15.2304 mL
20 mM	0.1523 mL	0.7615 mL	1.5230 mL	7.6152 mL

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Molecular Weight Calculator

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:

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 DMSO TargetMol | 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 DMSO TargetMol | reagent stock solution to 400 μL PEG300 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 ddH₂O TargetMol | 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.

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