MK-0812 Inhibitor

Solid. Powder

98.00%

Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent

469.54

DMSO: Soluble
(<1mg/ refers to the product slightly soluble or insoluble)

C24H34F3N3O3

CC(C1(C(N2CCC3=NC=C(C(F)(F)F)C=C3C2)=O)CCC(NC4CCOCC4OC)C1)C

624733-88-6

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

MK0812 (30mg/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].

Immunology/Inflammation; CCR