PF 06409577

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Cat.No. 6114 - PF 06409577 | C19H16ClNO3 | CAS No. 1467057-23-3
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
Reviews
Literature
Pathways

Biological Activity

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.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

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

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

Certificate of Analysis / Product Datasheet
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References

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


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Citations for PF 06409577

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Literature in this Area

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Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases

Pathways for PF 06409577

AMPK

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.