J-113863 is a potent, selective, non-peptide antagonist of CCR1 with IC50 of 0.9 and 5.8 nM for human and mouse CCR1 receptors, respectively. J-113863 is inactive against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. J-113863 is also a potent antagonist of the human CCR3 (IC50=0.58 nM), but a weak antagonist of the mouse CCR3 (IC50=460 nM). J-113863 improved paw inflammation and joint damage, and dramatically decreased cell infiltration into joints. J-113863 did not inhibit IL-2 or DTH, but reduced plasma TNFα levels in LPS-treated mice. J-113863 prevents the progression of in collagen-induced arthritis (CIA) model.
