Abstract: In this study, plasma, urine and fecal samples were collected from rats after intragastric administration of novel insulin sensitizer Zg02 (20 mg·kg^-1). The ultra-performance liquid chromatography-quadrupole-time-of-flight-tandem mass spectrometry (UPLC-Q-TOF/MS^E) techniques was used to obtain the molecular ion and mass spectrometry fragment ion information of the compound, and the metabolites were quickly analyzed by combining with UNIFI metabolite software. The results showed that a total of 12 metabolites were inferred in rats after a single gavage of Zg02 (20 mg·kg^-1), including 5, 7 and 11 metabolites in plasma, urine and feces (including cross-analysis), and the metabolic pathways were mainly glucuronidation and glucosylation. All animal protocols were approved by the Animal Ethics Committee of Guizhou Medical University (No. 2100856).