1173022-16-6

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 (IC₅₀ = 0.36 μM). It inhibits the related CCR1 receptor with an IC₅₀ value of 17.8 μM and inhibits adrenergic α_1a, α_1d, and 5HT_1A receptors with IC₅₀ values of 0.13, 0.32, and 47 μM, respectively. RS 102895 prevents chemotaxis of THP-1 cells (IC₅₀ = 1.7 μM) when MCP-1 is presented as a chemoattractant.

RS 102895 Hydrochloride is used as a leukocyte infiltrate marker for rosacea diagnosis.

CCR2: 360 nM (IC₅₀); CCR1: 17800 nM (IC₅₀); Human α_1a receptor: 130 nM (IC₅₀); Human α_1d receptor: 320 nM (IC₅₀); 5HT-1a receptor: 470 nM (IC₅₀)

Desiccate at RT

[1] T MIRZADEGAN. Identification of the binding site for a novel class of CCR2b chemokine receptor antagonists: binding to a common chemokine receptor motif within the helical bundle.[J]. The Journal of Biological Chemistry, 2000, 275 33: 25562-25571. DOI: 10.1074/jbc.m000692200