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MK-6892

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Catalog No. TQ0108Cas No. 917910-45-3

MK-6892 is a selective and full agonist for the high-affinity nicotinic acid receptor GPR109A (Ki: 4 nM; GTPγS EC50: 16 nM).

MK-6892

MK-6892

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Purity: 99.67%
Catalog No. TQ0108Cas No. 917910-45-3
MK-6892 is a selective and full agonist for the high-affinity nicotinic acid receptor GPR109A (Ki: 4 nM; GTPγS EC50: 16 nM).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$88In StockIn Stock
5 mg$198In StockIn Stock
10 mg$297In StockIn Stock
25 mg$497In StockIn Stock
50 mg$689In StockIn Stock
100 mg$987-In Stock
200 mg$1,330-In Stock
1 mL x 10 mM (in DMSO)$226In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.67%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
MK-6892 is a selective and full agonist for the high-affinity nicotinic acid receptor GPR109A (Ki: 4 nM; GTPγS EC50: 16 nM).
Targets&IC50
GPR109A:16 nM (EC50), GPR109A:4 nM (Ki)
In vitro
MK-6892 effectively induces the internalization of GPR109A in U2OS β-arrestin2-RrGFP cells and demonstrates a potent EC50 of 74 nM in calcium mobilization assays [2].
In vivo
MK-6892 is administered orally to WT and nicotinic acid (NA) receptor null mice on a C57Bl/6 genetic background. Following a 100 mg/kg dose, blood levels of MK-6892 reach 229 μM in WT mice and 148 μM in NA receptor null mice after 15 minutes, significantly exceeding the in vitro EC50 (240 nM). MK-6892 effectively suppresses plasma FFA in WT mice, but not in NA receptor null mice, indicating NA receptor-dependent FFA reduction [1].
Chemical Properties
Molecular Weight386.4
FormulaC19H22N4O5
Cas No.917910-45-3
SmilesCC(C)(Cc1nc(no1)-c1ccc(O)cn1)C(=O)NC1=C(CCCC1)C(O)=O
Relative Density.no data available
Storage & Solubility Information
StorageIn solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 45 mg/mL (116.46 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.18 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
1mg5mg10mg50mg
1 mM2.5880 mL12.9400 mL25.8799 mL129.3996 mL
5 mM0.5176 mL2.5880 mL5.1760 mL25.8799 mL
10 mM0.2588 mL1.2940 mL2.5880 mL12.9400 mL
20 mM0.1294 mL0.6470 mL1.2940 mL6.4700 mL
50 mM0.0518 mL0.2588 mL0.5176 mL2.5880 mL
100 mM0.0259 mL0.1294 mL0.2588 mL1.2940 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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
mg/kg
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μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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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

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