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Dihydromunduletone

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Catalog No. T11044Cas No. 674786-20-0
Alias DHM

Dihydromunduletone (DHM) is an adhesion G protein-coupled receptor (aGPCR) antagonist that acts as a chemical probe for the inhibition of GPR56 and GPR114/ADGRG5, which have similar tethered agonists.

Dihydromunduletone

Dihydromunduletone

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Purity: 99.96%
Catalog No. T11044Alias DHMCas No. 674786-20-0
Dihydromunduletone (DHM) is an adhesion G protein-coupled receptor (aGPCR) antagonist that acts as a chemical probe for the inhibition of GPR56 and GPR114/ADGRG5, which have similar tethered agonists.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$3117-10 days7-10 days
5 mg$7837-10 days7-10 days
1 mL x 10 mM (in DMSO)$8617-10 days7-10 days
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.96%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
Dihydromunduletone (DHM) is an adhesion G protein-coupled receptor (aGPCR) antagonist that acts as a chemical probe for the inhibition of GPR56 and GPR114/ADGRG5, which have similar tethered agonists.
Targets&IC50
GPR56:20.9 μM
In vitro
Assays commence with the addition of [35S]GTPγS, and the rates of aGPCR-stimulated G protein activation (Gα binding to [35S]GTPγS) are assessed with or without added compounds. Dihydromunduletone (DHM) significantly inhibits the kinetics of GPR56 7TM-stimulated G13 GTPγS binding, reducing activation by over 75%. At 50 μM DHM maximally inhibits GPR56 and dramatically reduces GPR114 7TM-stimulated Gs activity, but fails to inhibit GPR110 7TM stimulation of Gq GTPγS binding. Cells transfected with GPR56 A386M 7TM show concentration-dependent inhibition of P7 peptide-induced luciferase activity by DHM. Additionally, 3 μM DHM blunts P7 peptide activation at all concentrations. In conclusion, DHM antagonizes synthetic-peptide and tethered-peptide agonist-mediated aGPCR activation in isolated membranes and HEK293T cell-based assays but does not inhibit basal receptor signaling.
SynonymsDHM
Chemical Properties
Molecular Weight424.49
FormulaC25H28O6
Cas No.674786-20-0
SmilesO(C)C1=C2C(=CC=C1CC(=O)C=3C=C4C(=CC3O)OC(C)(C)C(O)C4)OC(C)(C)C=C2
Relative Density.1.223 g/cm3 (Predicted)
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 20 mg/mL (47.12 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2 mg/mL (4.71 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 mM2.3558 mL11.7788 mL23.5577 mL117.7884 mL
5 mM0.4712 mL2.3558 mL4.7115 mL23.5577 mL
10 mM0.2356 mL1.1779 mL2.3558 mL11.7788 mL
20 mM0.1178 mL0.5889 mL1.1779 mL5.8894 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

Dose Conversion

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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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