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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 Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $311 | 7-10 days | 7-10 days | |
| 5 mg | $783 | 7-10 days | 7-10 days | |
| 1 mL x 10 mM (in DMSO) | $861 | 7-10 days | 7-10 days |
| 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. |
| Synonyms | DHM |
| Molecular Weight | 424.49 |
| Formula | C25H28O6 |
| Cas No. | 674786-20-0 |
| Smiles | O(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) |
| Color | White |
| Appearance | Solid |
| Storage | store 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 recommeded. 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
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