JNJ-41443532

JNJ-41443532 (CCR2 antagonist 5) is a selective, orally active hCCR2 inhibitor with good binding affinity (IC50=37 nM) and potent functional antagonism (chemotaxis IC50=30 nM). JNJ-41443532 displays a Ki of 9.6 µM for mCCR2 binding. JNJ-41443532 can be used in the research of inflammatory disease.

JNJ-41443532 (compound 8d) 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].
JNJ-41443532 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].
JNJ-41443532 has amendable oral bioavailability in dogs and primates. Pharmacokinetic parameters (p.o.)^[1]:

Species	Dose (mg/kg)	Cmax (ng/mL)	AUClast (h*ng/mL)	Oral bioavailability (%)
dogs	6.7	1617	5887	70.2
non-human primates	7.2	740	3061	25.4
mice	10	74	204	19
rats	10	100	416	15.3