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PF-249 is an allosteric activator of AMP-activated protein kinase β1 (AMPKβ1) heterotrimers (EC50s = 8 and 6 nM for human AMPK α1β1γ1 and -α2β1γ1, respectively).1,2 It is selective for AMPK α1β1γ1 and -α2β1γ1 over AMPK α1β2γ1, -α2β2γ1, and -α2β2γ3 at 40 µM and a panel of receptors, channels, and phosphodiesterases at 10 µM.1,2 PF-249 decreases proteinuria and improves kidney function in an obese ZSF1 rat model of diabetic nephropathy in a dose-dependent manner.1
WARNING This product is not for human or veterinary use.
1. Selective activation of AMPK β1-
2. Acyl glucuronide metabolites of 6-