ZLN005 is a small molecule transcriptional regulator of peroxisome proliferator-activated receptor-γ coactivator-1α (PGC-1α). It stimulates the expression of PGC-1α and downstream genes in skeletal muscle cells, improving glucose utilization and fatty acid oxidation at a concentration of 20 μM. ZLN005 increases fat oxidation and improves the glucose tolerance, pyruvate tolerance, and insulin sensitivity of diabetic db/db mice.