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Beschreibung

A cis-diamidocyclohexyl urea compound that potently competes against MCP-1 binding to CCR2 (IC50 = 5.1 nM) and effectively inhibits MCP-1/CCR2-mediated PBMCs Ca+2 flux and chemotaxis (IC50 = 18 and 1 nM, respectively), while showing much less effect against eotaxin binding to CCR3 (37% inhibition at 10 µ,M). Mutageneis analysis indicates CCR2 Thr292 is critical in maintaining the high affinity antagonist binding.