Catalog No.: PC-20733Not For Human Use, Lab Use Only.
AMG487 (AMG 487, VUF10085) is a potent and selective orally bioavailable chemokine (C-X-C motif) receptor 3 (CXCR3) antagonist with IC50 of 8 nM for inhibiting 125I-IP-10 binding.
AMG487 (AMG 487, VUF10085) is a potent and selective orally bioavailable chemokine (C-X-C motif) receptor 3 (CXCR3) antagonist with IC50 of 8 nM for inhibiting 125I-IP-10 binding.
AMG 487 also inhibits binding of 125I-ITAC to CXCR3 with an IC50 value of 8.2 nM.
AMG487 inhibits CXCR3-mediated cell migration by the three CXCR3 chemokines (IP-10 IC50 = 8 nM, ITAC IC50 = 15 nM, and MIG IC50 = 36 nM).
AMG487 inhibits calcium mobilization in response to ITAC (IC50 = 5 nM).
AMG487 exhibits good potency in binding and functional assays and good in vivo pharmacokinetic properties across species. AMG487 is a potent inhibitor of cellular recruitment in vivo using a bleomycine-mouse model.
