1349637-14-4

CP-289,503 is an inhibitor of the complement C5a receptor with an IC50 of 1 μM. C5a acts as an activator of leukocytes and phagocytes during complement system activation. The C5a receptor can bind to C5a, which can stimulate the upregulation of cell surface integrins and degranulation of inflammatory cells, leading to endothelial cell damage. C5a receptor inhibitors can block C5a signaling and inhibit a variety of inflammatory diseases[1].

[1] Blagg J, et al. Small, non-peptide C5a receptor antagonists: part 1. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5601-4. DOI:10.1016/j.bmcl.2008.08.106