| Description | INCB 3284 is an orally available, selective and high affinity chemokine receptor 2 (CCR2) antagonist that inhibits monocyte chemotactic protein 1 from interacting with hCCR2.INCB 3284 is used in the study of hemorrhagic shock. |
| In vitro | INCB3284 在拮抗单核细胞趋化蛋白-1与 hCCR2 结合方面表现出 3.7 nM的 IC50，在拮抗趋化活性方面的 IC50 为4.7 nM，在抑制 hERG 钾电流方面的 IC50 为84 μM[1]。 |
| In vivo | INCB 3284 (1 mg/kg/天，腹腔注射) 或 C021 显著改善了 AOM 治疗小鼠的神经系统结局，减少了小胶质细胞的活化，减少了 ERK1/2 的磷酸化，并减轻了 AOM 诱导的细胞因子上调[2]。 |
| Target activity | MCP-1-hCCR2:3.7 nM, K+ channel (hERG):84 μM |
| molecular weight | 520.54 |
| Molecular formula | C26H31F3N4O4 |
| CAS | 887401-92-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: < 0.1 mg/mL (insoluble) DMSO: 60 mg/mL (115.26 mM), Sonication is recommended. |
| References | 1. Xue CB, et al. Discovery of INCB3284, a Potent, Selective, and Orally Bioavailable hCCR2 Antagonist. ACS Med Chem Lett. 2011 Mar 31;2(6):450-4. 2. McMillin M, et al. Neuronal CCL2 is upregulated during hepatic encephalopathy and contributes to microglia activation and neurological decline. J Neuroinflammation. 2014 Jul 10;11:121. |