1. GPCR/G Protein Immunology/Inflammation
  2. CCR
  3. MK-0812 Succinate

MK-0812 Succinate 

Cat. No.: HY-50669A Purity: 99.94%
COA Handling Instructions

MK-0812 Succinate is a potent and selective CCR2 antagonist with high affinity at CCR2.

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
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 233 In-stock
Solution
10 mM * 1 mL in DMSO USD 233 In-stock
Solid
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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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

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Description

MK-0812 Succinate is a potent and selective CCR2 antagonist with high affinity at CCR2.

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]

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

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].

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

Clinical Trial
Molecular Weight

587.63

Appearance

Solid

Formula

C28H40F3N3O7

CAS No.
SMILES

O=C([C@]1(C(C)C)C[C@H](N[C@H]2CCOC[C@H]2OC)CC1)N3CCC(N=CC(C(F)(F)F)=C4)=C4C3.O=C(O)CCC(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.25 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (4.25 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.25 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.94%

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
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MK-0812 Succinate Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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MK-0812 Succinate
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