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MK-0812

Catalog No. TQ0182   CAS 624733-88-6

MK-0812 is an effective and specific CCR2 antagonist.

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MK-0812 Chemical Structure
MK-0812, CAS 624733-88-6
Pack Size Availability Price/USD Quantity
1 mg 35 days $ 183.00
5 mg 35 days $ 720.00
10 mg 35 days $ 1,340.00
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Biological Description
Chemical Properties
Storage & Solubility Information
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].
Kinase Assay 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].
Animal Research 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
Formula C24H34F3N3O3
CAS No. 624733-88-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: Soluble

TargetMolReferences and Literature

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.

TargetMolCitations

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.

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Keywords

MK-0812 624733-88-6 Immunology/Inflammation Microbiology/Virology CCR MK 0812 MK0812 inhibitor inhibit

 

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