SLU-PP-332 is a potent, selective, and orally bioavailable small-molecule agonist of estrogen-related receptor α (ERRα), a nuclear receptor and orphan transcription factor that plays a central role in regulating mitochondrial biogenesis, oxidative phosphorylation, and energy metabolism in high-energy-demanding tissues such as skeletal muscle, heart, and brown adipose tissue. SLU-PP-332 exhibits an EC₅₀ of approximately 98 nM for ERRα activation with >100-fold selectivity over ERRβ/γ and no significant activity against the classical estrogen receptors ERα and ERβ, thereby avoiding estrogenic side effects. In preclinical models, acute and chronic administration of SLU-PP-332 induces ERRα-dependent gene expression (e.g., Pgc-1α, Acadm, Idh3a), promotes mitochondrial function, increases oxidative muscle fibers, enhances exercise endurance capacity (up to ~70% improvement in treadmill running time in mice), stimulates fat utilization, and improves insulin sensitivity without affecting body weight. These properties position SLU-PP-332 as a promising “exercise mimetic” compound with potential therapeutic applications in metabolic disorders (obesity, type 2 diabetes), muscle-wasting conditions, and age-related decline in physical performance.