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    Immunology/Inflammation
  2. CCR
  3. MK-0812

MK-0812 

Cat. No.: HY-50669 Purity: 99.75%
Handling Instructions

MK-0812 is a potent and selective CCR2 antagonist with low nM affinity for CCR2.

For research use only. We do not sell to patients.

MK-0812 Chemical Structure

MK-0812 Chemical Structure

CAS No. : 624733-88-6

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Description

MK-0812 is a potent and selective CCR2 antagonist with low nM affinity for CCR2.

IC50 & Target[1]

CCR2

 

In Vitro

MK-0812 completely blocks all MCP-1 mediated response in a concentration dependent manner, with an IC50 of 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). In fact, the antagonist not only completely blocks the shape change response to exogenous MCP-1, but also results in 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[1] MK0812 is a potent and selective small molecule CCR2 antagonist[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

MK-0812 is administered by continuous i.v. infusion to maintain a constant level of the drug in blood[1]. Administration of MK0812 at 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

469.54

Formula

C₂₄H₃₄F₃N₃O₃

CAS No.

624733-88-6

SMILES

O=C([[email protected]]1(C(C)C)C[[email protected]](N[[email protected]]2CCOC[[email protected]]2OC)CC1)N3CCC(N=CC(C(F)(F)F)=C4)=C4C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
References
Kinase Assay
[1]

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 which, 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% para-formaldehyde) 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 scatter measurements[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Mice[2]
Female BALB/c mice are used between 8 and 10 weeks of age. SCH563705 or 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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

MK-0812MK0812MK 0812CCRCC chemokine receptorInhibitorinhibitorinhibit

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