O-304 is a first-in-class, orally available pan-AMPK activator, which increasesAMPK activity by suppressing the dephosphorylation of pAMPK. O-304 exhibits a great potential as a drug to treat type 2 diabetes (T2D) and associated cardiovascular complications [1][2].
AMPK activated protein kinase (AMPK), a master regulator of energy homeostasis, is activated in response to an energy shortage. When pathological conditions cause ATP levels to fall, AMPK is activated to restore cellular energy homeostasis[1]. O-304 is a first-in-class, orally available pan-AMPK activator, which increases AMPK activity by suppressing the dephosphorylation of pAMPK. It exhibits a great potential as a drug to treat type 2 diabetes (T2D) and associated cardiovascular complications. Mice fed with a high-fat diet (HFD), denoted DIO mice, were treated by oral gavage with vehicle, O304, Metformin, or O304+Metformin (100 mg/kg/day) each for 8 weeks. O304 and O304+Metformin, but not Metformin, averted the HFD-provoked increase in fasted glucose and plasma insulin levels and inhibited insulin resistance[2]. Postoperative pain mice models made by incision in the left plantar hindpaw were treated by oral gavage with vehicle, metformin 200 mg/kg, O304 200 mg/kg and O304 200 mg/kg plus metformin 200 mg/kg, for 3 days. O304 or metformin increased von Frey thresholds (reduced mechanical hypersensitivity) in plantar incision mice compared to vehicle-treated incision mice[3].
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