BX-513

BX-513 is a highly potent and selective CCR1 antagonist. BX-513 effectively inhibits the binding of radiolabeled MIP-1α and RANTES to CCR1, with K_i values of 40 nM and 60 nM, respectively. BX-513 suppresses MIP-1α-induced extracellular acidification, MIP-1α- and RANTES-induced intracellular calcium mobilization, as well as MIP-1α- and RANTES-induced migration of peripheral blood mononuclear cells. BX-513 can be used for the research of rheumatoid arthritis and multiple sclerosis^[1]. In Vitro:BX-513 (Compound 1) (30-1000 nM) dose-dependently inhibits MIP-1α-induced extracellular acidification in THP-1 cells, with an IC₅₀ of 124 nM, and also suppresses RANTES-induced acidification in these cells^[1].
BX-513 (100-1000 nM) inhibits CCR1-expressing HEK 293 cells in a dose-dependent manner, with an IC₅₀ of approximately 200 nM. This compound has no intrinsic agonist activity, exerts reversible inhibitory effects, and also inhibits RANTES-induced intracellular Ca²⁺ mobilization in these cells^[1].
BX-513 (20-2000 nM) dose-dependently inhibits MIP-1α- and RANTES-induced chemotaxis of human peripheral blood mononuclear cells (PBMCs), without affecting migration induced by other chemokines^[1].