This invention discloses a pre-targeting probe
assembly for
in vivo unstable iron
pool imaging, its preparation method, and its application. The pre-targeting probe
assembly includes Fe... 2+ Response paramagnetic probe GdEpTz and
fluorescent reporter probe 2E-Tco-Hcy, Fe 2+ Response paramagnetic probe GdEpTz with Fe 2+ Following interaction with endogenous proteins, free radicals are generated and covalent cross-linking occurs, significantly increasing the
longitudinal relaxation rate (r1) by approximately 104.1%. Simultaneously,
tetrazine-based Tz is efficiently enriched in the
lesion region. The enriched Tz captures the fluorescent
signal reporter probe 2E-Tco-Hcy via a highly efficient IEDDA bioorthogonal reaction, triggering a 155.5-fold significant enhancement of the
fluorescence signal. This invention introduces a bioorthogonal pre-targeting strategy based on the reverse
electron demand Diels-
Alder (IEDDA) reaction, aiming to achieve Fe in deep tissues through the organic integration of "target-induced activation" and "bioorthogonal
chemistry." 2+ Dynamically changing,
highly selective, and high-contrast synchronous
visual monitoring.