Selective transcriptional regulator of peroxisome proliferator–activated receptor-γ coactivator-1α (PGC-1α). ZLN005 selectively stimulated the expression of PGC-1α and downstream genes in skeletal muscle cells, and led to changes in glucose uptake, and fatty acid oxidation in L6 myotubes in a AMPK dependent manner. Since ZLN 005 did not increase the expression of the PGC-1α gene in rat primary hepatocytes, it is hypothesized that expression of PGC-1α was regulated in a cell type–specific manner. ZLN005 exerts promising therapeutic effects for treating type 2 diabetes, as PGC-1α is a powerful transcriptional coregulator of GLUT4 and mitochondrial genes, a crucial player in the field of glucose uptake in skeletal muscle.