TSPO Ligand

Tosylate-DPA-714 is a GMP-grade precursor for the radiosynthesis of DPA-714 (HY-122607). It crosses the blood-brain barrier and exhibits steroidogenic activity. DPA-714 is a specific ligand for the 18 kDa translocator protein (TSPO) with a K_i of 7.0 nM. Tosylate-DPA-714 is safe and does not bind to central benzodiazepine receptors (benzodiazepine receptor). As a radiolabeling precursor, Tosylate-DPA-714 reacts with ¹⁸F via nucleophilic aliphatic substitution to form ¹⁸F-DPA-714, enabling specific targeted binding to TSPO. ¹⁸F-DPA-714 accurately reflects the level of neuroinflammation mediated by microglial activation, and is used for PET molecular imaging of neurological diseases such as Alzheimer's disease and multiple sclerosis.

TSPO ligand-2 is a ligand of AUTAC1. AUTAC1 contains an p-fluorobenzylguanine (FBnG) and a Fumagillol moiety, which can silence endogenous MetAP2 in HeLa cells.

DPA-713 is a blood-brain barrier-permeable, specific translocator protein (TSPO) ligand. DPA-713 binds exclusively to TSPO without interacting with central benzodiazepine receptors; its binding can be competitively displaced by excess unlabeled TSPO ligands. After ¹¹C labeling, DPA-713 enables sensitive quantitative analysis of TSPO expression associated with microglial activation, allowing differentiation between normal and pathological brain tissues. DPA-713 can be used in studies related to neuroinflammation, neurodegenerative diseases, and recently onset schizophrenia.

NZ-66 is a ULK1-Recruiting Chimera (ULKREC) and heterobifunctional chimeric molecule composed of a BL-918-derived ULK1 agonist linked to a mitochondrial outer membrane-targeting TSPO ligand via a six-carbon hexane linker. NZ-66 is a mitophagy inducer recruits ULK1 to mitochondria to induce ULK1-dependent mitophagy, enhanced by mitochondrial insult, independently of the PRKN/PINK axis. NZ-66 can be used for the research of parkinson’s disease.