MK-0812

Cat. No.: HY-50669 Purity: 98.01%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

For research use only. We do not sell to patients.

MK-0812 Chemical Structure

CAS No. : 624733-88-6

Size	Price	Stock	Quantity
1 mg	USD 72	In-stock	Estimated Time of Arrival: December 31
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		Get quote
100 mg		Get quote

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Other Forms of MK-0812:

MK-0812 Succinate In-stock

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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

IC₅₀ & Target^[1]

CCR2

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].

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

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^-Ly6C^hi 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 Ly6C^hi monocytes and a corresponding elevation in the CCR2 ligand CCL2^[2].

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

Clinical Trial

Molecular Weight

469.54

Formula

C₂₄H₃₄F₃N₃O₃

CAS No.

624733-88-6

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (212.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1297 mL	10.6487 mL	21.2974 mL
5 mM	0.4259 mL	2.1297 mL	4.2595 mL
10 mM	0.2130 mL	1.0649 mL	2.1297 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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 (5.32 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% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.32 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).

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: 99.75%

Select Batch:

Data Sheet (280 KB) SDS (252 KB)

COA (257 KB) HNMR (192 KB) LCMS (307 KB)

Handling Instructions (2659 KB)

References

[1]. 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]

[2]. 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]

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]	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^-Ly6C^hi 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	[1]. 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] [2]. 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]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.1297 mL	10.6487 mL	21.2974 mL	53.2436 mL
	5 mM	0.4259 mL	2.1297 mL	4.2595 mL	10.6487 mL
	10 mM	0.2130 mL	1.0649 mL	2.1297 mL	5.3244 mL
	15 mM	0.1420 mL	0.7099 mL	1.4198 mL	3.5496 mL
	20 mM	0.1065 mL	0.5324 mL	1.0649 mL	2.6622 mL
	25 mM	0.0852 mL	0.4259 mL	0.8519 mL	2.1297 mL
	30 mM	0.0710 mL	0.3550 mL	0.7099 mL	1.7748 mL
	40 mM	0.0532 mL	0.2662 mL	0.5324 mL	1.3311 mL
	50 mM	0.0426 mL	0.2130 mL	0.4259 mL	1.0649 mL
	60 mM	0.0355 mL	0.1775 mL	0.3550 mL	0.8874 mL
	80 mM	0.0266 mL	0.1331 mL	0.2662 mL	0.6655 mL
	100 mM	0.0213 mL	0.1065 mL	0.2130 mL	0.5324 mL

MK-0812 Related Classifications

Inflammation/Immunology Endocrinology

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.

Keywords:

MK-0812624733-88-6MK0812MK 0812CCRCC chemokine receptorInhibitorinhibitorinhibit

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