AG-041R is primarily used in research settings for its potent and selective agonist activity at the gastrin-releasing peptide receptor (GRPR). It is utilized to study cellular signaling pathways associated with GRPR activation, particularly in neuroscience and oncology research. Due to the overexpression of GRPR in certain cancers such as prostate, breast, and lung cancers, AG-041R serves as a valuable tool compound for investigating tumor growth mechanisms and evaluating targeted therapeutic strategies. It has also been employed in imaging studies, where it can be labeled with radiotracers for positron emission tomography (PET) to detect and monitor cancer progression. Its high selectivity minimizes off-target effects, making it suitable for precise biological probing in vitro and in vivo models.