| Description | MK-0812 Succinate is an effective and selective CCR2 antagonist. |
| In vitro | MK-0812 not only fully blocks the shape change response to exogenous MCP-1 but also causes a monocyte forward scatter measurement below unstimulated or basal levels. The addition of MK-0812 to rhesus blood also inhibits MCP-1 induced monocyte shape change. The IC50 for MK-0812 in whole blood assays is 8 nM. MK-0812 fully blocks all MCP-1 mediated response in a concentration-dependent manner (IC50: 3.2 nM). This value is similar to the potency observed for the inhibition of 125I-MCP-1 binding by MK-0812 on isolated monocytes (IC50: 4.5 nM) [2]. |
| In vivo | MK-0812 is administered by continuous i.v. infusion to maintain a constant level of the drug in the blood. MK-0812 treatment induces a dose-dependent reduction in circulating Ly6Chi monocytes and a corresponding elevation in the CCR2 ligand CCL2. MK-0812 (30 mg/kg, p.o.) decreases the frequency of Ly6G-Ly6Chi monocytes in the peripheral blood, while no impact on circulating Ly6G+Ly6C+ neutrophil frequency is observed [1][2]. |
| Target activity | MCP-1:4.5 nM |
| molecular weight | 587.63 |
| Molecular formula | C28H40F3N3O7 |
| CAS | 851916-42-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 28 mg/mL (47.65 mM) |
| References | 1. Min SH, et al. Pharmacological targeting reveals distinct roles for CXCR2/CXCR1 and CCR2 in a mouse model of arthritis.Biochem Biophys Res Commun. 2010 Jan 1;391(1):1080-6. 2. Wisniewski T, et al. Assessment of chemokine receptor function on monocytes in whole blood: In vitro and ex vivo evaluations of a CCR2 antagonist.J Immunol Methods. 2010 Jan 31;352(1-2):101-10. |