BMS-681

A potent and orally bioavailable dual antagonist of CCR2 and CCR5 with binding IC50 of 0.7 nM and 2.4 nM, respectively; exhibits high selectivity against other chemokine receptors and GPCRs; 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); suitable for use in both murine and monkey models of inflammation.

References 1. Zheng Y, et al. Nature. 2016 Dec 15;540(7633):458-461. 2. Carter PH, et al. ACS Med Chem Lett. 2015 Mar 4;6(4):439-44. View Related Products by Target Chemokine Receptor (CCR and CXCR)