OS-01 is an AMP-activated protein kinase (AMPK) activator that modulates cellular energy homeostasis and metabolic function. AMPK, a central regulator of energy balance, is activated in response to low intracellular ATP levels, enhancing glucose uptake, fatty acid oxidation, and mitochondrial biogenesis. OS-01 stimulates AMPK phosphorylation, leading to increased ATP production, improved insulin sensitivity, and enhanced autophagic flux, thereby promoting cellular repair and longevity. This compound has been shown to mitigate oxidative stress by downregulating reactive oxygen species (ROS) and inflammatory cytokines, reducing cellular damage and aging-related dysfunction. Additionally, OS-01 enhances endurance by optimizing energy substrate utilization and preserving glycogen stores during exercise. It plays a protective role in renal and cardiovascular systems by attenuating fibrosis, reducing endothelial dysfunction, and improving mitochondrial efficiency. Preclinical studies suggest its potential in managing metabolic disorders, including type 2 diabetes, obesity, and cardiovascular diseases, by improving glucose homeostasis and reducing insulin resistance. Furthermore, OS-01’s activation of autophagy contributes to neuroprotection, reducing age-related neurodegeneration. Its multifaceted mechanism positions it as a promising candidate for therapeutic intervention in metabolic and age-related diseases.