Abaucin

RS102895 is a potent CCR2 antagonist, with an IC₅₀ of 360 nM, and shows no effect on CCR1. IC50 & Target:IC50: 360 nM (CCR2)^[1] In Vitro: RS102895 is a potent CCR2 antagonist, with an IC₅₀ of 360 nM, and shows no effect on CCR1. RS102895 also inhibits human α1a and 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 (ECM) protein expression by inhibition of CCR2 at 10 μM, and obviously blocks fibronectin and type IV collagen protein expression in high glucose (HG)-stimulated mesangial cells (MCs) at 1 or 10 μM. RS102895 (10 μM) also abrogates the increased TGF-1 levels in MCs treated with MCP-1^[2]. In Vivo: RS102895 (3 g/L) causes progressive decrease in pain threshold in rats with bone cancer pain (BCP) at day 3-9 after surgery via intrathecal injection, but the pain threshold increases after 12 days. RS102895 also potently reverses the pattern of NR2B, nNOS, and SIGIRR expression in spinal cord^[3].