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PF-06409577 AMPK activator

Name: PF-06409577
Brand: Selleck Chemicals
SKU: S8335
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S8335

PF-06409577 is an orally bioavailable AMPK activator with EC50 of 7 nM for α1β1γ1 in the TR-FRET assay and it shows no detectable inhibition of hERG in a patch-clamp assay (100 μM) and was not an inhibitor (IC50 > 100 μM) of the microsomal activities of major human cytochrome P450 isoforms.

Chemical Structure

Molecular Weight: 341.79

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Quality Control

Batch: S833501 DMSO]100 mg/mL]false]Ethanol]68 mg/mL]false]Water]Insoluble]false Purity: 99.44%

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.44

Related Targets	PI3K Akt mTOR GSK-3 ATM/ATR DNA-PK PDPK1 PTEN PP2A PDK
Other AMPK Inhibitors	Dorsomorphin Dihydrochloride Dorsomorphin (Compound C) AICAR (Acadesine) A-769662 GSK621 WZ4003 ex229 (compound 991) Phenformin HCl BAY-3827 HTH-01-015

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (292.57 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 68 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (14.63mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.85mg/ml (14.19mM)	Taking the 1 mL working solution as an example, add 50 μL of 97 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.69mg/ml (2.02mM)	Taking the 1 mL working solution as an example, add 50 μL of 13.8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Average weight of animals: g

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	341.79	Formula	C₁₉H₁₆ClNO₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1467057-23-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1CC(C1)(C2=CC=C(C=C2)C3=C(C=C4C(=C3)C(=CN4)C(=O)O)Cl)O

Mechanism of Action

Targets/IC₅₀/Ki	AMPK α2β1γ1 6.8 nM(EC50) AMPK α1β1γ1 7 nM(EC50)
In vitro	PF-06409577 activates α1β1γ1 and α2β1γ1 AMPK isoforms with EC50 of 7.0 nM and 6.8 nM but this compound was much less active against α1β2γ1/α2β2γ1/α2β2γ3 AMPK isoforms with EC50 greater 4000 nM.
In vivo	PF-06409577 exhibits efficacy in a preclinical model of diabetic nephropathy. It exhibits high plasma protein binding in rat (plasma unbound fraction, fu,p = 0.0044), dog (fu,p = 0.028), monkey (fu,p = 0.032), and human (fu,p = 0.017). Following iv administration, this compound demonstrates moderate plasma clearance (CLp) in rats (22.6 mL/min/kg), dogs (12.9 mL/min/kg), and monkeys (8.57 mL/min/kg) and was well distributed with steady state distribution volumes (Vdss) ranging from 0.846-3.15 L/kg. Following oral administration of crystalline material in 0.5% methylcellulose suspension, it is rapidly absorbed (Tmax = 0.25-1.20 h) in rats, dogs, and monkeys. The corresponding oral bioavailability (F) values in rats, dogs, and monkeys, were 15%, 100%, and 59%, respectively. This chemical is subject to a higher degree of first pass intestinal glucuronidation in the rat (relative to other preclinical species and human).
References	[1] https://pubmed.ncbi.nlm.nih.gov/28665353/ [2] https://pubmed.ncbi.nlm.nih.gov/27490827/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02286882	Terminated	Healthy	Pfizer	November 2014	Phase 1

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