GPR183 antagonist 32 is potent, selective antagonist of GPR183 (EBI2) with IC50 of 8.6/12.1 nM (human/mouse β-arrestin), respectively.
GPR183 antagonist 32 blocks human U937 and Th17 cell migration with IC50 values of 5.5 nM and 3.8 nM, respectively.
GPR183 antagonist 32 does not show any cytotoxicity to human hepatocytes, with an IC50 value of more than 150 μM.
GPR183 antagonist 32 potently antagonizes 7α,25-OHC-induced calcium mobilization in vitro (IC50=31.3 nM).
GPR183 antagonist 32 (0.1, 0.3, and 1.0 mg/kg) reduced inflammation, bone erosion, pannus formation, and cartilage damage, downregulated the expression of multiple CIA-associated genes in the paw joints of CIA mice.
