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Catalpol hexapropionate (CP-6) was designed and synthesized as anti-aging drug. In order to investigate the behavior of CP-6 in simulated gastric juice, ultra-high performance liquid chromatography-electrospray ionization-high resolution mass spectrometry was used to determinate the components produced in simulated gastric conditions. Six metabolites were identified with the possible metabolic processes proposed. Hydrolysis may be the main metabolic pathways. The relative contents of CP-6 and its metabolites were determined using their extractive ion chromatograms. The results show that the relative content of CP-6 is rapidly decreased about 15% during the first 0.5 h and generally stable after 0.5 h. The mainly produced metabolites are catalpol penta-propionate (CP-5), catalpol and a spot of catalpol tetra-propionate (CP-4), catalpol tri-propionate (CP-3), catalpol dipropionate (CP-2) and catalpol propionate (CP-1). The metabolitic process of CP-6 may be an hydrolysis under acid conditions. The research results can provide useful information for development and utilization of CP-6 as a pharmaceutical preparation.