biostudies-literatureHa KNHLBI NIH HHSNational Heart, Lung, and Blood InstituteNational Natural Science Foundation of China2225-2232https://www.ebi.ac.uk/biostudies/studies/S-EPMC8767556biostudies-literatureUnknown6(6)Platelets play a prominent role in multiple diseases, in particular arterial and venous thrombosis and also in atherosclerosis and cancer. To advance the <i>in vivo</i> study of the biological activity of this cell type from a basic experimental focus to a clinical focus, new translatable platelet-specific molecular imaging agents are required. Herein, we report the development of a near-infrared fluorescence probe based upon tirofiban, a clinically approved small-molecule glycoprotein IIb/IIIa inhibitor (GPIIb/IIIa). Through <i>in vitro</i> experiments with human platelets and <i>in vivo</i> ones in a murine model of deep-vein thrombosis, we demonstrate the avidity of the generated probe for activated platelets, with the added benefit of a short blood half-life, thereby enabling rapid <i>ACS sensors<i>In Vivo</i> Platelet Detection Using a Glycoprotein IIb/IIIa-Targeted Near-Infrared Fluorescence Imaging Probe.PMC8767556R01HL133153R01 HL144550R01HL144550R01 HL133153R01HL150538R01 HL122388R01 HL150538R01 HL137913R01HL137913R01HL12223881800431R01 HL122238Li WKawamura YJaffer FAMauskapf AZheng XMcCarthy JRHa KOrii MHilderbrand SAKessinger CWfalse<i>In Vivo</i> Platelet Detection Using a Glycoprotein IIb/IIIa-Targeted Near-Infrared Fluorescence Imaging Probe.Platelets play a prominent role in multiple diseases, in particular arterial and venous thrombosis and also in atherosclerosis and cancer. To advance the <i>in vivo</i> study of the biological activity of this cell type from a basic experimental focus to a clinical focus, new translatable platelet-specific molecular imaging agents are required. Herein, we report the development of a near-infrared fluorescence probe based upon tirofiban, a clinically approved small-molecule glycoprotein IIb/IIIa inhibitor (GPIIb/IIIa). Through <i>in vitro</i> experiments with human platelets and <i>in vivo</i> ones in a murine model of deep-vein thrombosis, we demonstrate the avidity of the generated probe for activated platelets, with the added benefit of a short blood half-life, thereby enabling rapid <i>2021-01-01T00:00:00Z2021 Jun2025-04-25T22:22:16.996Z2025-04-06T09:04:48.094ZS-EPMC87675563405690310.1021/acssensors.1c00124