Allosteric AMP-activated protein kinase (AMPK) activator; allosterically stimulates active AMPK heterotrimers, increasing the activity of α
1 by 1.5-fold and α
1 by 1.7-fold (EC50
values are 0.42 and 0.95 μ
M, respectively). Inhibits dephosphorylation of AMPK Thr-172 by PP2Cα
. Stimulates glucose uptake and fatty acid oxidation without increasing the ADP/ATP ratio. Also decreases fatty acid synthesis and glucose output in primary hepatocytes. Improves glucose tolerance and decreases cholesterol content in db/db
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Novel small-molecule AMPK activator orally exerts beneficial effects on diabetic db/db mice.
Li et al.
Novel small-molecule AMP-activated protein kinase allosteric activator with beneficial effects in db/db mice.
Zhang et al.
PLoS One, 2013;8:e72092