摘要:SummaryReliable and sensitive detection of lipase activity is essential for the early diagnosis and monitoring of acute pancreatitis or progression of digestive diseases. However, the available fluorescent probes for detection of lipase activity are only implemented in a hexane-water two-phase system due to the nature of heterogeneous catalysis of lipase, thus limiting their applications in direct imaging of lipase activity in living cells and tissues. Here we designed and synthesized a “turn on” fluorescent probe CPP based on self-assembled micelles for hydrolysis of lipase. The CPP probe exhibits high selectivity and excellent sensitivity for the detection of lipase in such a homogeneous system and is successfully applied for monitoring lipase activity in pancreatic AR42J cells, tissues, and serums. Taken together, the fluorescent CPP probe not only provides a tool for diagnostic potential in pancreatic disease but also demonstrates an application potential for micelle self-assembly-based development of biological probes.Graphical AbstractDisplay OmittedHighlights•A CPP probe is synthesized via acylation of fluorescent CP-OH and palmitoyl chloride•Hydrophobic CPP probe forms self-assembled micelles with hydrophilic lipase•The CPP selectively detects heterogeneous –catalysis of lipase activity in cells•The fluorescent CPP has developmental potential for diagnostic use in diseasesBiophysical Chemistry; Biocatalysis; Biophysics