Abstract: An in vitro glycation model was set up by glucose and human serum albumin (HSA) based on Maillard Reaction. HPLC-ESI TOF MS and ¹⁸O-labeling technique were employed to quantify glycation level of peptides cleaved from HSA. In order to screen glucose-sensitive peptides for being diabetic biomarker-candidates, the in vitro glycation model was set up and confirmed, and eleven biomarker-candidates were screened based on the model by HPLC-ESI TOF MS quantification. Eleven glucose-sensitive peptides were screened for being biomarker-candidates, which needs to be verified in clinical trials in the future.