强效选择性人 CCR2 拮抗剂
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.
Buntinx et al (2008) 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 J.Pharmacol.Exp.Ther. 327 1 PMID:18599682
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