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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, CAS 624733-88-6

Pack Size	Availability	Price/USD
1 mg	4-5 weeks	$ 183.00
5 mg	4-5 weeks	$ 720.00
10 mg	4-5 weeks	$ 1,340.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

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

References 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.

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.

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Keywords

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

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