cyclosporin H

Cyclosporin H is a non-immunosuppressive cyclic undecapeptide and a diastereomer of the well-known immunosuppressant Cyclosporin A. Unlike Cyclosporin A, which binds to cyclophilin to inhibit calcineurin, Cyclosporin H lacks significant calcineurin-inhibiting activity. Instead, it acts as a potent and selective antagonist of the Formyl Peptide Receptor 1 (FPR1), a G protein-coupled receptor primarily expressed on neutrophils and macrophages. FPR1 plays a critical role in the innate immune response by sensing N-formyl peptides derived from bacteria or damaged mitochondria. By blocking FPR1, Cyclosporin H inhibits leukocyte chemotaxis and the production of reactive oxygen species. Recent research has demonstrated its potential protective effects in sepsis-associated acute kidney injury (SA-AKI) by modulating FPR1 signaling and inhibiting pyroptosis, making it a valuable pharmacological tool for studying FPR1-mediated inflammatory processes.

Other names

Cyclosporine HD-MeVal-1-cyclosporinD-MeVal1-cyclosporinD-MeVal 1-cyclosporin