| Description | MK-0812 is an effective and specific CCR2 antagonist. |
| In vitro | MK-0812 completely 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). 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 [1]. |
| In vivo | MK0812 (30 mg/kg, p.o.) reduces the frequency of Ly6G-Ly6Chi monocytes in the peripheral blood, while no impact on circulating Ly6G+Ly6C+ neutrophil frequency is observed. In addition, MK0812 treatment causes a dose-dependent reduction in circulating Ly6Chi monocytes and a corresponding elevation in the CCR2 ligand CCL2 [2]. |
| Animal experiments | Female BALB/c mice are used between 8 and 10 weeks of age. MK0812 are administered in a 0.4% MC solution by 30 mg/kg oral gavage (p.o.). Two hours later, the frequency of CD11b+Ly6G-Ly6Chi monocytes and CD11b+Ly6G+Ly6C+ neutrophils is determined by flow cytometry [2]. |
| molecular weight | 469.54 |
| Molecular formula | C24H34F3N3O3 |
| CAS | 624733-88-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: Soluble |
| References | 1. 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. 2. 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. |
| Citations | 1. Sugiyama S, Yumimoto K, Fujinuma S, et al.Identification of effective CCR2 inhibitors for cancer therapy using humanized mice.The Journal of Biochemistry.2023: mvad086. |