2. Epigenetics PI3K/Akt/mTOR
  3. AMPK
  4. PF-739

PF-739 is an orally active and non-selective activator of AMPK. PF-739 activates 12 heterotrimeric AMPK complexes and significantly reduces the level of glucose in plasma complexes.

For research use only. We do not sell to patients.

PF-739 Chemical Structure

PF-739 Chemical Structure

CAS No. : 1852452-14-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 275 In-stock
Solution
10 mM * 1 mL in DMSO USD 275 In-stock
Solid
5 mg USD 250 In-stock
10 mg USD 425 In-stock
25 mg USD 893 In-stock
50 mg USD 1518 In-stock
100 mg USD 2580 In-stock
200 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

PF-739 Related Antibodies

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View All AMPK Isoform Specific Products:

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NUAK1 NUAK2 AMPK AMPK α1β1γ1 AMPK α2β1γ1 AMPK α1β2γ1 AMPK α2β2γ1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PF-739 is an orally active and non-selective activator of AMPK. PF-739 activates 12 heterotrimeric AMPK complexes and significantly reduces the level of glucose in plasma complexes[1][2].

IC50 & Target[1]

AMPK α1β1γ1

8.99 nM (EC50)

AMPK α1β2γ1

126 nM (EC50)

AMPK α2β1γ1

5.23 nM (EC50)

AMPK α2β2γ1

42.2 nM (EC50)

In Vitro

PF-739 activates α2β1γ1, α2β2γ1, α1β1γ1 and α1β2γ1 with EC50 values of 5.23 nM, 42.2 nM, 8.99 nM and 126 nM, respectively[1].
PF-739 (0-1000 nM) increases the phosphorylation of AMPK substrate in primary rat hepatocytes and myotubes of primary human cardiac cell line with dose-dependent manner[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PF-739 Related Antibodies
In Vivo

PF-739 (30-1000 mg/kg; p.o. or s.c.; single does) effectively activates AMPK in liver cells and skeletal muscle and reduces plasma glucose level in C57BL/6 mice[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 mice[2].
Dosage: 30, 100, 300 or 1000 mg/kg.
Administration: Oral gavage or subcutaneous injection; single does.
Result: Increased AMPK activity in skeletal muscle, AMPK phosphorylation in liver tissue and the expression of transcription factors Ppargc1a, Nr4a1, Nr4a3 in glucose metabolism pathway, and decreased plasma insulin and blood glucose.
Molecular Weight

442.89

Formula

C23H23ClN2O5
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O[C@H]1[C@]([H])([C@@]2(OC1)[H])OC[C@H]2OC3=NC4=CC(C5=CC=C(C=C5)C6(CC6)CO)=C(C=C4N3)Cl
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
In Vitro: 

DMSO : 100 mg/mL (225.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2579 mL 11.2895 mL 22.5790 mL
5 mM 0.4516 mL 2.2579 mL 4.5158 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (5.64 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (5.64 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2579 mL 11.2895 mL 22.5790 mL 56.4474 mL
5 mM 0.4516 mL 2.2579 mL 4.5158 mL 11.2895 mL
10 mM 0.2258 mL 1.1289 mL 2.2579 mL 5.6447 mL
15 mM 0.1505 mL 0.7526 mL 1.5053 mL 3.7632 mL
20 mM 0.1129 mL 0.5645 mL 1.1289 mL 2.8224 mL
25 mM 0.0903 mL 0.4516 mL 0.9032 mL 2.2579 mL
30 mM 0.0753 mL 0.3763 mL 0.7526 mL 1.8816 mL
40 mM 0.0564 mL 0.2822 mL 0.5645 mL 1.4112 mL
50 mM 0.0452 mL 0.2258 mL 0.4516 mL 1.1289 mL
60 mM 0.0376 mL 0.1882 mL 0.3763 mL 0.9408 mL
80 mM 0.0282 mL 0.1411 mL 0.2822 mL 0.7056 mL
100 mM 0.0226 mL 0.1129 mL 0.2258 mL 0.5645 mL
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PF-739 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PF-7391852452-14-2PF739PF 739AMPKAMP-activated protein kinaseMiceα2β1γ1α2β2γ1α1β1γ1α1β2γ1Inhibitorinhibitorinhibit

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