Description
The chemokine CCL2, also known as monocyte chemotactic protein-1 (MCP-1), stimulates leukocyte chemotaxis to sites of inflammation
via signaling through the MCP-1 receptor, CCR2. RS 102895 is a spiropiperidine compound that acts as a CCR2 antagonist (IC
50 = 0.36 μM). It inhibits the related CCR1 receptor with an IC
50 value of 17.8 μM and inhibits adrenergic α
1a, α
1d, and 5HT
1A receptors with IC
50 values of 0.13, 0.32, and 47 μM, respectively. RS 102895 prevents chemotaxis of THP-1 cells (IC
50 = 1.7 μM) when MCP-1 is presented as a chemoattractant.
