Hepatotoxicity　is　a　serious　problem　faced　by　thousands　of　clinical　drugs,　and　drug-induced　liver　injury　(DILI)　caused　by　chronic　administration　or　overdose　has　become　a　major　biosafety　issue.　However,　the　near-infrared　(NIR)　fluorescent　probes　currently　used　for　liver　injury　detection　still　suffer　from　poor　liver　targeting　ability　and　low　sensitivity.　Enzyme-activated　fluorogenic　probes　with　powerful　in　situ　targeting　ability　are　the　key　to　improving　the　imaging　effect　of　liver　injury.　Herein,　we　rationally　designed　a　leucine　aminopeptidase　(LAP)　activated　fluorogenic　probe　hCy-CA-LAP,　which　greatly　improved　the　hepatocyte-targeting　capability　by　introducing　a　cholic　acid　group.　The　probe　hCy-CA-LAP　is　converted　into　a　high-emission　hCy-CA　fluorophore　in　the　presence　of　LAP,　showing　high　selectivity,　high　sensitivity　and　low　detection　limit　(0.0067　U　mL(-1))　for　LAP,　and　successfully　realizes　the　sensitive　detection　of　small　fluctuations　of　LAP　in　living　cells.　Moreover,　the　probe　can　achieve　effective　in　situ　accumulation　in　the　liver,　thereby　achieving　precise　imaging　and　evaluation　of　two　different　types　of　drug-induced　hepatotoxicity　in　vivo.　Therefore,　the　probe　hCy-CA-LAP　may　be　a　potential　tool　for　exploring　the　roles　of　LAP　and　evaluating　the　degree　of　DILI.