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Dihydromunduletone
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
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 Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $179 | In Stock |
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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.Product Introduction
Bioactivity
Chemical Properties
| 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. |
| Alias | DHM |
| Molecular Weight | 424.49 |
| Formula | C25H28O6 |
| Cas No. | 674786-20-0 |
Storage & Solubility Information
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 20 mg/mL (47.12 mM), Sonication is recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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