1. GPCR/G Protein
    Immunology/Inflammation
  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
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg USD 180 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 336 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 1176 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 1860 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
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

Description

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

IC50 & Target

CCR2[1]

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].

References
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
[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]

MK0812 is prepared in 0.4% methylcellulose (MC) (Mice)[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
Molecular Weight

587.63

Formula

C₂₈H₄₀F₃N₃O₇

CAS No.

851916-42-2

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

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

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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Product Name:
MK-0812 Succinate
Cat. No.:
HY-50669A
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