MK-0812 is a dual antagonist of the CCR2 and CCR5 receptors that can alleviate adipose inflammation in ob/ob mice.

MK-0812 以浓度依赖的方式完全阻断所有 MCP-1 介导的应答，IC50 为 3.2 nM。
MK-0812 结合单核细胞的 MCP-1，IC50 为 4.5 nM。[1]

MK-0812 （10 mg/kg/小鼠）饲喂，增加了 ob/ob 小鼠的 eWAT 质量，有效抑制 ob/ob 脂肪组织中巨噬细胞浸润。[3]

Human whole blood is collected in EDTA tubes and used within 1 h of blood collection. For antagonist treated samples, blood (200 μL) is pre-incubated with MK-0812 (0.1% final DMSO concentration) for 30 min at room temperature. After this, 20 μL of FITC conjugated anti-CD14 antibody and 4 μL of chemokine or buffer is added to each sample and mixed lightly. An aliquot (100 μL) of the blood mixture is incubated for 10 min at 37°C immediately placed on ice and lightly fixed with 250 μL of ice-cold fixative (49 mL PBS, 1.0 mL 4% paraformaldehyde) for 1 min. Red blood cells are lysed by adding 1.0 mL of ice-cold lysis solution (0.15 M NH4Cl2, 10 mM sodium bicarbonate, and 1 mM EDTA), and incubated for 20 min on ice. After complete lysis of red blood cells, 100 μL of 4% para-formaldehyde is added and the samples are analyzed by flow cytometry for forward scattering measurements [1].

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].