Cat. No.: HY-103683

PF-06409577

Name: PF-06409577
Brand: MedChemExpress
SKU: HY-103683
Price: 77.00 USD
Availability: InStock
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PF-06409577 is a potent and selective allosteric activator of AMPK α1β1γ1 isoform with an EC₅₀ of 7 nM.

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

Purity : 99.83%
CAS No.: 1467057-23-3
Formula: C₁₉H₁₆ClNO₃
Molecular Weight:341.79

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

PF-06409577 Chemical Structure

CAS No.: 1467057-23-3

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

PF-06409577 is a potent and selective allosteric activator of AMPK α1β1γ1 isoform with an EC₅₀ of 7 nM.

IC₅₀ & Target

^[1]

AMPK α1β1γ1

7 nM (EC₅₀)

All AMPK Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	>30000 nM Compound: 7	Agonist activity at human recombinant 5-HT2b receptor expressed in CHO cells measured after 30 mins by HTRF assay Agonist activity at human recombinant 5-HT2b receptor expressed in CHO cells measured after 30 mins by HTRF assay	[PMID: 27490827]
Sf9	EC₅₀	>40 μM Compound: 29; PF-06409577	Activation of rat hepatocytes AMPK alpha1/beta2/gamma1 expressed in baculovirus infected Sf9 cells Activation of rat hepatocytes AMPK alpha1/beta2/gamma1 expressed in baculovirus infected Sf9 cells	[PMID: 31930920]
Sf9	EC₅₀	0.007 μM Compound: 29; PF-06409577	Activation of rat hepatocytes AMPK alpha1/beta1/gamma1 expressed in baculovirus infected Sf9 cells Activation of rat hepatocytes AMPK alpha1/beta1/gamma1 expressed in baculovirus infected Sf9 cells	[PMID: 31930920]
Vero	CC₅₀	586.4 μM Compound: 54; PF-06409577	Cytotoxicity against African green monkey Vero cells after 48 hrs by Cell Titer Glo luminescent cell viability assay Cytotoxicity against African green monkey Vero cells after 48 hrs by Cell Titer Glo luminescent cell viability assay	[PMID: 31549836]
Vero	CC₅₀	923.7 μM Compound: 54; PF-06409577	Cytotoxicity against African green monkey Vero cells after 24 hrs by Cell Titer Glo luminescent cell viability assay Cytotoxicity against African green monkey Vero cells after 24 hrs by Cell Titer Glo luminescent cell viability assay	[PMID: 31549836]
Vero	EC₅₀	2.6 μM Compound: 54; PF-06409577	Activation of AMPK in African green monkey Vero cells infected with Zika virus PA259459 assessed as antiviral activity measured 24 hrs post infection by plaque assay Activation of AMPK in African green monkey Vero cells infected with Zika virus PA259459 assessed as antiviral activity measured 24 hrs post infection by plaque assay	[PMID: 31549836]

In Vitro

PF-06409577 possesses similar potency toward the human and rat α1β1γ1 isoforms. In broad panel screening against other receptors, channels, PDEs and kinases, PF-06409577 exhibits minimal off-target pharmacology. PF-06409577 shows no detectable inhibition of hERG in a patch-clamp assay (100 μM) and is not an inhibitor (IC₅₀>100 μM) of the microsomal activities of major human cytochrome P450 isoforms^[1].

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

In Vivo

PF-06409577 demonstrates moderate plasma clearance in rats, dogs, and monkeys, and is well distributed with steady state distribution volume. Following oral administration of crystalline PF-06409577 in 0.5% methylcellulose suspension, PF-06409577 is rapidly absorbed in rats, dogs, and monkeys. The corresponding oral bioavailability values in rats, dogs, and monkeys, are 15%, 100%, and 59%, respectively. Dose responsive increases in pAMPK relative to total AMPK (tAMPK) in whole kidney tissue are observed with a maximal 3.8-fold response at 300 mg/kg PF-06409577 treatment^[1]. Oral administration of PF-06409577 (10, 30, and 100 mg/kg QD) results in dose-dependent reductions in proteinuria in the obese ZSF1 animals, with greater than 2-fold reduction in 24-hour urinary albumin loss compared to vehicle control after 60 days of treatment^[1].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1467057-23-3
Appearance Solid
Molecular Weight 341.79
Formula C₁₉H₁₆ClNO₃
Color White to off-white
SMILES

O=C(C1=CNC2=C1C=C(C3=CC=C(C4(O)CCC4)C=C3)C(Cl)=C2)O
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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mBio

The vitamin D receptor is essential for the replication of pseudorabies virus. [Abstract]

2024 Dec 11;15(12):e0213724. PMID: 39475231

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (292.58 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.9258 mL

14.6289 mL

29.2577 mL

5 mM

0.5852 mL

2.9258 mL

5.8515 mL

10 mM

0.2926 mL

1.4629 mL

2.9258 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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: ≥ 2.08 mg/mL (6.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

Protocol 2

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

Solubility: ≥ 2.08 mg/mL (6.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (6.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Cameron KO, et al. Discovery and Preclinical Characterization of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy. J Med Chem. 2016 Sep 8;59(17):8068-81. [Content Brief]

[2]. Salatto CT, et al. Selective Activation of AMPK β1-Containing Isoforms Improves Kidney Function in a Rat Model of Diabetic Nephropathy. J Pharmacol Exp Ther. 2017 May;361(2):303-311. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.9258 mL	14.6289 mL	29.2577 mL	73.1443 mL
	5 mM	0.5852 mL	2.9258 mL	5.8515 mL	14.6289 mL
	10 mM	0.2926 mL	1.4629 mL	2.9258 mL	7.3144 mL
	15 mM	0.1951 mL	0.9753 mL	1.9505 mL	4.8763 mL
	20 mM	0.1463 mL	0.7314 mL	1.4629 mL	3.6572 mL
	25 mM	0.1170 mL	0.5852 mL	1.1703 mL	2.9258 mL
	30 mM	0.0975 mL	0.4876 mL	0.9753 mL	2.4381 mL
	40 mM	0.0731 mL	0.3657 mL	0.7314 mL	1.8286 mL
	50 mM	0.0585 mL	0.2926 mL	0.5852 mL	1.4629 mL
	60 mM	0.0488 mL	0.2438 mL	0.4876 mL	1.2191 mL
	80 mM	0.0366 mL	0.1829 mL	0.3657 mL	0.9143 mL
	100 mM	0.0293 mL	0.1463 mL	0.2926 mL	0.7314 mL

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PF-06409577

Publications Citing Use of MedChemExpress (MCE) PF-06409577

All AMPK Isoforms