BMS CCR2 22

BMS CCR2 22 is a potent, specific and high affinity CC-type chemokine receptor 2 (CCR2) antagonist with excellent binding affinity (binding IC₅₀ of 5.1 nM) and potent functional antagonism (calcium flux IC₅₀ of 18 nM and chemotaxis IC₅₀ of 1 nM)^[1][2]. In Vitro: BMS CCR2 22 (Compound 22) has binding affinity for wild-type and E291A mutants with IC₅₀ values of 7.5 nM and 3.7 nM, respectively^[1]. BMS CCR2 22 prevents both the binding and the internalization of fluorescently labeled hMCP-1_AF647 internalization in human monocytes. BMS CCR2 22 inhibits the internalization of hMCP1_AF647 with an IC₅₀ value of approximately 2 nM^[2].
The addition of BMS CCR2 22 (0.1-10 μM; 24 h), cenicriviroc (CVC) or a combination of both BMS CCR2 22 and MVC to human aortic endothelial cells (HAoECs) prior to MCP-1 stimulation do not alter E-selectin, ICAM-1, or CD99 cell surface expression. Incubation of HAoECs with BMS CCR2 22 before MCP-1 significantly increases VCAM-1 and PECAM1 cell surface levels (from 72.8 to 160% and from 97.2 and 127%, respectively)^[3].