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18F-FB(ePEG12)12-Ex4 is a fluorine-18 labeled radiopharmaceutical designed for positron emission tomography (PET) imaging of the glucagon-like peptide-1 receptor (GLP-1R). The molecule consists of the GLP-1R agonist Exendin-4, a 39-amino acid peptide, which is conjugated to a [18F]fluorobenzoyl (FB) prosthetic group via a 12-unit polyethylene glycol (ePEG12) linker. The conjugation typically occurs at the Lysine-12 (K12) residue of the peptide, which preserves the binding affinity for GLP-1R. This tracer is primarily developed for the localization of insulinomas (insulin-secreting tumors) and the non-invasive quantification of pancreatic beta-cell mass. The inclusion of the PEG linker enhances the tracer's pharmacokinetic properties by increasing hydrophilicity, which reduces non-specific uptake in the liver and promotes rapid renal clearance, thereby improving the target-to-background ratio in clinical imaging.
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