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PF-249

Name: PF-249
Brand: TargetMol
SKU: T24626
Price: 41 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T24626Cas No. 1467059-70-6

Alias PF-06685249, PF06685249, PF 06685249

PF-249 (PF-06685249) is a β1-selective AMPK with an EC50 of 12 nM for AMPK α1β1γ1 and can be used in studies about diabetic nephropathy.

PF-249

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Purity: 97.01%

Catalog No. T24626Alias PF-06685249, PF06685249, PF 06685249Cas No. 1467059-70-6

PF-249 (PF-06685249) is a β1-selective AMPK with an EC50 of 12 nM for AMPK α1β1γ1 and can be used in studies about diabetic nephropathy.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$41	In Stock	In Stock
5 mg	$98	In Stock	In Stock
10 mg	$158	In Stock	In Stock
25 mg	$263	In Stock	In Stock
50 mg	$382	In Stock	In Stock
100 mg	$536	-	In Stock
200 mg	$736	-	In Stock
1 mL x 10 mM (in DMSO)	$107	In Stock	In 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:97.01%

Appearance:Solid

Color:White

Resource Download

COA LCMS HNMR

Product Introduction

PF-249 AI Summary

PF-249 is an allosteric activator of human AMPK alpha1/beta1/gamma1. It has a half-maximal effective concentration (EC50) of approximately 11.7 nM to 12.0 nM, as determined by various assays, including a 33P-based assay and one using a SAMS peptide derived from ACC-1. The compound demonstrates high binding affinity to AMPK alpha1/beta1/gamma1 with dissociation constants (Kd) ranging from 13.6 nM to 14.0 nM. It exhibits substantial solubility in sodium phosphate buffer at pH 7.4 and activates AMPK in cryopreserved human hepatocytes with an EC50 of 280.0 nM. Additionally, it shows moderate activity in reducing 14C-2-acetic acid incorporation in recombinant AMPKbeta1 with an IC50 of 420.0 nM. Pharmacokinetically, PF-249 has moderate to high oral bioavailability in rat and cynomolgus monkey models, with varying clearance rates and half-lives, indicating species-specific differences in metabolism. The compound also exhibits substrate activity at various transporters and enzymes in both human and rat cell models..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	PF-249 (PF-06685249) is a β1-selective AMPK with an EC50 of 12 nM for AMPK α1β1γ1 and can be used in studies about diabetic nephropathy.
Targets&IC50	AMPK α1β1γ1:12 nM (EC50)
Synonyms	PF-06685249, PF06685249, PF 06685249

Chemical Properties

Molecular Weight	345.78
Formula	C₁₇H₁₆ClN₃O₃
Cas No.	1467059-70-6
Smiles	COc1nc(ccc1-c1cc2c(c[nH]c2cc1Cl)C(O)=O)N(C)C
Relative Density.	1.400 g/cm3 (Predicted)

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 90 mg/mL (260.28 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.8920 mL	14.4601 mL	28.9201 mL	144.6006 mL
5 mM	0.5784 mL	2.8920 mL	5.7840 mL	28.9201 mL
10 mM	0.2892 mL	1.4460 mL	2.8920 mL	14.4601 mL
20 mM	0.1446 mL	0.7230 mL	1.4460 mL	7.2300 mL
50 mM	0.0578 mL	0.2892 mL	0.5784 mL	2.8920 mL
100 mM	0.0289 mL	0.1446 mL	0.2892 mL	1.4460 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:

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