RS102895 is a potent CCR2 antagonist (IC50: 360 nM) and shows no effect on CCR1.

α1A-adrenoceptor:130 nM, α1D-adrenoceptor (human):320 nM, CCR2:360 nM, 5-HT1A:470 nM

RS102895 also inhibits human α1a, α1d receptors, rat brain cortex 5HT1a receptor in cells with IC50s of 130, 320, 470 nM, respectively. RS102895 suppresses wild type and D284N mutant MCP-1 receptor (IC50, 550 nM and 568 nM, respectively), less potently inhibits D284A MCP-1 receptor (IC50, 1892 nM), and has no effects on E291A, E291Q, D284A/E291A or D284N/E291Q (IC50, >100,000?nM) [1]. RS102895 ameliorates the increased extracellular matrix protein expression by inhibition of CCR2 at 10 μM and obviously blocks fibronectin and type IV collagen protein expression in high glucose-stimulated mesangial cells (MCs) at 1 or 10 μM. RS102895 (10 μM) also abrogate the increased TGF-1 levels in MCs treated with MCP-1 [2].

RS102895 at a concentration of 3 g/L progressively lowers the pain threshold in rats experiencing bone cancer pain (BCP) from days 3 to 9 post-surgery through intrathecal administration, with the threshold rising again after day 12. Additionally, RS102895 effectively alters the expression levels of NR2B, nNOS, and SIGIRR in the spinal cord.