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MK-0812

Name: MK-0812
Brand: TargetMol
SKU: TQ0182
Rating: 4.5 (1 reviews)

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Catalog No. TQ0182Cas No. 624733-88-6

Alias MK0812

MK-0812 is a dual antagonist of the CCR2 and CCR5 receptors that can alleviate adipose inflammation in ob/ob mice.

MK-0812

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Catalog No. TQ0182Alias MK0812Cas No. 624733-88-6

MK-0812 is a dual antagonist of the CCR2 and CCR5 receptors that can alleviate adipose inflammation in ob/ob mice.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$100	35 days	35 days
5 mg	$243	35 days	35 days
10 mg	$436	35 days	35 days

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Appearance:Solid

Color:White

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Product Introduction

Bioactivity

Description	MK-0812 is a dual antagonist of the CCR2 and CCR5 receptors that can alleviate adipose inflammation in ob/ob mice.
In vitro	MK-0812 completely blocks all McP-1-mediated responses in a concentration-dependent manner, with an IC50 of 3.2 nM. MK-0812 binds MCP-1 of monocytes with an IC50 of 4.5 nM. [1]
In vivo	Feeding MK-0812 (10 mg/kg/ mouse) increased eWAT quality of ob/ob mice and effectively inhibited macrophage infiltration in ob/ob adipose tissue. [3]
Kinase Assay	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 this, 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% paraformaldehyde) 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 scattering measurements [1].
Animal Research	Female BALB/c mice are used between 8 and 10 weeks of age. 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 [2].
Synonyms	MK0812

Chemical Properties

Molecular Weight	469.54
Formula	C₂₄H₃₄F₃N₃O₃
Cas No.	624733-88-6
Smiles	C(=O)([C@]1([C@H](C)C)C[C@H](N[C@@H]2[C@H](OC)COCC2)CC1)N3CC=4C(CC3)=NC=C(C(F)(F)F)C4
Relative Density.	1.24 g/cm3

Storage & Solubility Information

Storage

store at low temperature | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 80 mg/mL (170.38 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (7.03 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1297 mL	10.6487 mL	21.2974 mL	106.4872 mL
5 mM	0.4259 mL	2.1297 mL	4.2595 mL	21.2974 mL
10 mM	0.2130 mL	1.0649 mL	2.1297 mL	10.6487 mL
20 mM	0.1065 mL	0.5324 mL	1.0649 mL	5.3244 mL
50 mM	0.0426 mL	0.2130 mL	0.4259 mL	2.1297 mL
100 mM	0.0213 mL	0.1065 mL	0.2130 mL	1.0649 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc