Potent and selective allosteric activator of AMPK (EC50
values are 7 and >40000 nM for AMPKα
1 and AMPKα
1, respectively). Exhibits minimal off target effects on a panel of receptors, ion channels, PDEs and kinases. Demonstrates efficacy in a preclinical model of diabetic nephropathy. Orally bioavailable.
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All Tocris products are intended for laboratory research use only.
Sold for research purposes under agreement from Pfizer Inc.
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
Cameron et al.