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 high affinity at 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 the United States
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 high affinity at CCR2 on human monocytes.

IC50 & Target[1]

CCR2

 

In Vitro

MK-0812 is a potent and selective CCR2 antagonist[1]. 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, MK-0812 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[2]

In Vivo

MK-0812 (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, MK-0812 treatment causes a dose-dependent reduction in circulating Ly6Chi monocytes and a corresponding elevation in the CCR2 ligand CCL2[1]. MK-0812 is administered by continuous i.v. infusion to maintain a constant level of the drug in blood[2].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : ≥ 32 mg/mL (54.46 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent 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.
References
Animal Administration
[1]

Mice[1]
Female BALB/c mice are used between 8 and 10 weeks of age. SCH563705 or MK-0812 are administered in a 0.4% methylcellulose (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[1]
.

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

Purity: 99.57%

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

Cat. No.: HY-50669A