| Description | CCR2 antagonist 4 (Teijin compound 1) is a potent and specific antagonist of CCR2(IC50s of 180 nM), and potently inhibits MCP-1-induced chemotaxis(IC50 of 24 nM). |
| In vivo | Vp-TSL 特异性靶向动脉粥样硬化斑块内皮细胞的 VCAM-1，而 CCR2 antagonist 4 在 ApoE 缺陷小鼠中减少了小鼠单核细胞/巨噬细胞系 (RAW 264.7) 对主动脉的粘附/浸润[3]。 |
| Target activity | CCR2b:180 nM |
| Synonyms | Teijin compound 1 |
| molecular weight | 439.86 |
| Molecular formula | C21H21ClF3N3O2 |
| CAS | 226226-39-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 50 mg/mL (113.67 mM) |
| References | 1. Moree WJ, et al. Potent antagonists of the CCR2b receptor. Part 3: SAR of the (R)-3-aminopyrrolidine series. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1869-73. 2. Hall SE, et al. Elucidation of binding sites of dual antagonists in the human chemokine receptors CCR2 and CCR5. Mol Pharmacol. 2009 Jun;75(6):1325-36. 3. Calin M, et al. VCAM-1 directed target-sensitive liposomes carrying CCR2 antagonists bind to activated endothelium and reduce adhesion and transmigration of monocytes. Eur J Pharm Biopharm. 2015 Jan;89:18-29. |