BMS-687681 (BMS-681) is a potent and orally bioavailable dual antagonist of CCR2 and CCR5 with binding IC50 of 0.7 nM and 2.4 nM, respectively.
BMS-681 exhibits high selectivity against other chemokine receptors and GPCRs.
BMS-681 shows CCR2 functional assays of monocyte chemotaxis (IC50=0.24 nM) and CD11b upregulation (whole blood IC50=4.7 nM), CCR5 functional assays of human T-cells (IC50=2.3 nM) and whole blood CCR5-mediated CD11b upregulation (IC50=4.3 nM),
BMS-681 is suitable for use in both murine and monkey models of inflammation.
