INCB3344，5MG，SML3924-5MG，Sigma

Biochem/physiol Actions

Orally active, potent and selective CCR2 antagonist in vitro and in vivo.
INCB3344 is an orally active, potent and selective CCR2 antagonist (human/mouse/rat/cynomolgus IC50 = 5.1/9.5/7.3/16 nM by competitive binding assays, IC50 = 3.8/7.8/2.7/6.2 nM by chemotaxis assays) with >100-fold selectivity over other homologous chemokine receptors. INCB3344 shows in vivo efficacy in a murine EAE model (thioglycolate-induced peritonitis in mice; 30-100 mg/kg bid. p.o. against peritoneal macrophage influx) and a rat adjuvant arthritis model (100 mg/kg bid. p.o. against adjuvant-induced macrophages infiltration of the joint).