MK-0812 Succinate

Name: MK-0812 Succinate
Brand: MedChemExpress
SKU: HY-50669A
Rating: 4.5 (1 reviews)

Cat. No.: HY-50669A Purity: 99.90%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 851916-42-2

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 233	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 233	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 180	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 336	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1176	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1860	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of MK-0812 Succinate:

MK-0812 Get quote

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View All CCR Isoform Specific Products:

View All Isoforms

CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

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^-Ly6C^hi 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 Ly6C^hi 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

Formula

C₂₈H₄₀F₃N₃O₇

CAS No.

851916-42-2

Appearance

Solid

Color

White to off-white

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.25 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.90%

Select Batch:

Data Sheet (277 KB) SDS (393 KB)

COA (254 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. 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. [Content Brief]

[2]. 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. [Content Brief]

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^-Ly6C^hi 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

[1]. 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. [Content Brief]

[2]. 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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7018 mL	8.5088 mL	17.0175 mL	42.5438 mL
	5 mM	0.3404 mL	1.7018 mL	3.4035 mL	8.5088 mL
	10 mM	0.1702 mL	0.8509 mL	1.7018 mL	4.2544 mL
	15 mM	0.1135 mL	0.5673 mL	1.1345 mL	2.8363 mL
	20 mM	0.0851 mL	0.4254 mL	0.8509 mL	2.1272 mL
	25 mM	0.0681 mL	0.3404 mL	0.6807 mL	1.7018 mL
	30 mM	0.0567 mL	0.2836 mL	0.5673 mL	1.4181 mL
	40 mM	0.0425 mL	0.2127 mL	0.4254 mL	1.0636 mL
	50 mM	0.0340 mL	0.1702 mL	0.3404 mL	0.8509 mL