CCR2 antagonist 5 (JNJ-41443532) is a selective and orally active hCCR2 inhibitor with good binding affinity (IC50=37 nM) and potent functional antagonism (chemotaxis IC50=30 nM).JNJ-41443532 binds mCCR2 with a Ki of 9.6 µM, which can be used to study inflammatory diseases and diabetes. diseases and diabetes.

CCR2 (mouse):9.6 μM (Ki), CCR2 (human):37 nM (IC50)

CCR2 antagonist 5 (compound 8d) has good CV safety profile. It does not induce dose-dependent or notable effects on most cardiohemodynamic, functional respiratory, and electrophysiological parameters up to 10 mg/kg (i.v.) with plasma level at 70 µM in an anesthetized dog.[1]
CCR2 antagonist 5 dose-dependently inhibits the influx of leukocytes, monocytes/macrophages, and T-lymphocytes into the peritoneal cavity with an ED50 of 3 mg/kg p.o. bid in a thioglycollate-induced peritonitis (TG) model.[1]
CCR2 antagonist 5 has amendable oral bioavailability in dogs and primates.[1]