Chemical Name:6-Methyl-1'-[2-(5-methyl-2-phenyl-4-oxazolyl)ethyl]-spi
ro[4H-3,1-benzoxazine-4,4'-piperidin]-2(1H)-one
Biological Activity:
Extremely selective CCR2 chemokine receptor
antagonist (IC50 values are 98 nM and > 100 μM for
inhibition of human recombinant CCR2b and CCR1 receptors respectively).
Inhibits MCP-1 chemotaxis (IC50 = 330 nM) and ischaemia-reperfusion
injury in kidneys.
Mirzadeganet al (2000)
Identification of the binding site for a novel class of CCR2b chemokine
receptor antagonists. J.Biol.Chem. 275 25562. Furuichiet
al (2003) CCR2 signaling contributes to ischemia-reperfusion injury in
kidney. J.Am.Soc.Nephrol. 14 2503. Kitagawaet al
(2004) Blockade of CCR2 ameliorates progressive fibrosis in kidney.
Am.J.Pathol. 165 237.
Potent CXCR2 antagonist that inhibits CINC-1-mediated but not C5a-mediated Ca2+ mobilisation (IC50 values are 3.4 and 6800 nM respectively). Inhibits CINC-induced chemotaxis & attenuates neutrophil accumulation in inflammatory lung injury in vivo.