Potent, noncompetitive human CCR2 antagonist; inhibits MCP-1-induced Ca2+
mobilization in hCCR2-CHO cells (IC50
= 13 nM). Exhibits selectivity for CCR2 over CCR1, CCR3-8 and CXCR1-3. Delays onset and reduces neurological signs in an experimental autoimmune encephalomyelitis model of multiple sclerosis in hCCR2 knock-in mice. Orally active.
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All Tocris products are intended for laboratory research use only.
Pharmacological profile of JNJ-27141491 [(S)-3-[3,4-difluorophenyl)-propyl]-5-isoxazol-5-yl-2-thioxo-2,3-dihydro-1H-imidazole-4-carboxyl acid methyl ester], as a noncompetitive and orally active antagonist of the human chemokine receptor
Buntinx et al.