1. GPCR/G Protein
  2. CCR

MK-0812 Succinate 

Cat. No.: HY-50669A Purity: 99.57%
Handling Instructions

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

For research use only. We do not sell to patients.
MK-0812 Succinate Chemical Structure

MK-0812 Succinate Chemical Structure

CAS No. : 851916-42-2

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 233 In-stock
5 mg USD 180 In-stock
10 mg USD 336 In-stock
50 mg USD 1176 In-stock
100 mg USD 1860 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Other Forms of MK-0812 Succinate:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References


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

IC50 & Target


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].

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].

Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 1.7018 mL 8.5088 mL 17.0175 mL
5 mM 0.3404 mL 1.7018 mL 3.4035 mL
10 mM 0.1702 mL 0.8509 mL 1.7018 mL
Please refer to the solubility information to select the appropriate solvent.
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 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

MK0812 is prepared in 0.4% methylcellulose (MC) (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.

Molecular Weight







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.O=C(O)CCC(O)=O

Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 32 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.57%

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