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PF 06409577

Cat. No. 6114 1 Citation Submit a Review Datasheet / COA / SDS
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Description: Potent and selective allosteric activator of AMPK
Chemical Name: 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic acid
Purity: ≥98% (HPLC)
Datasheet
Citations (1)
Reviews
Pathways (1)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for PF 06409577

PF 06409577 is a potent and selective allosteric activator of AMPK (EC50 values are 7 and >40000 nM for AMPKα1β1γ1 and AMPKα1β2γ1, respectively). Exhibits minimal off-target effects on a panel of receptors, ion channels, PDEs and kinases. Improves kidney function and reduces proteinuria in a preclinical model of diabetic nephropathy. Orally bioavailable.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Compound Libraries for PF 06409577

PF 06409577 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.

Technical Data for PF 06409577

M. Wt 341.79
Formula C19H16ClNO3
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 1467057-23-3
PubChem ID 71748255
InChI Key FHQXLWCFSUSXBF-UHFFFAOYSA-N
Smiles O=C(O)C1=CNC2=CC(Cl)=C(C3=CC=C(C4(CCC4)O)C=C3)C=C21

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for PF 06409577

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 34.18 100
ethanol 6.84 20

Preparing Stock Solutions for PF 06409577

The following data is based on the product molecular weight 341.79. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.93 mL 14.63 mL 29.26 mL
5 mM 0.59 mL 2.93 mL 5.85 mL
10 mM 0.29 mL 1.46 mL 2.93 mL
50 mM 0.06 mL 0.29 mL 0.59 mL

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Product Datasheets for PF 06409577

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References for PF 06409577

References are publications that support the biological activity of the product.

Cameron et al (2016) 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 diab J.Med.Chem. 59 8068 PMID: 27490827

Salatto et al (2017) Selective activation of AMPK β1-containing isoforms improves kidney function in a rat model of diabetic nephropathy. J.Pharmacol.Exp.Ther. 361 303 PMID: 28289077

If you know of a relevant reference for PF 06409577, please let us know.

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1 Citation for PF 06409577

Citations are publications that use Tocris products. Selected citations for PF 06409577 include:

Smith et al (2019) An ErbB2/c-Src axis links bioenergetics with PRC2 translation to drive epigenetic reprogramming and mammary tumorigenesis. Nat Commun 10 2901 PMID: 31263101

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Pathways for PF 06409577

AMPK Signaling Pathway

AMPK Signaling Pathway

AMPK signaling pathway plays an important role in the cellular reponse to low levels of available ATP, often caused by stresses such as heat shock, ischemia or hypoxia.