| Bioactivity | JNJ-27141491 is a selective, noncompetitive and orally active functional antagonist of human CCR2[1]. |
| Invitro | JNJ-27141491 抑制 MCP-1 诱导的 [35S]GTPγS 与 hCCR2-CHO 细胞膜的结合 (IC50=38±9 nM)，并减少 MCP-1 诱导的 Ca2+ 动员，在 hCCR2-CHO 细胞的 IC50 为 13±1 nM，在 THP-1 细胞的 IC50 为 13±2 nM 和在人血单核细胞的 IC50 为 43±4 nM。JNJ-27141491 也抑制人 PBMC 对 MCP-1 的趋化作用，其 IC50 值为 97±16 nM[1]。JNJ-27141491 与 MCP-1 和 hCCR2 的结合竞争，并作为 CCR2 受体的非竞争性拮抗剂[1]。 |
| In Vivo | JNJ-27141491 (5-40 mg/kg; oral; once or twice daily) 抑制单核细胞和中性粒细胞招募到转基因 hCCR2 敲入小鼠的肺泡空气空间[1]。JNJ-27141491 (20 mg/kg; oral; daily for 16 days) 在转基因 CCR2 小鼠中延迟实验性自身免疫性脑脊髓炎 (EAE)[1]。 Animal Model: |
| Name | JNJ-27141491 |
| CAS | 871313-59-6 |
| Formula | C17H15F2N3O3S |
| Molar Mass | 379.38 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Buntinx M, et al. 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 CCR2. J Pharmacol Exp Ther. 2008 Oct;327(1):1-9. |