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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

🥰Excellent
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.
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1 mg170 €In Stock
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Purity:99.96%
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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.
AliasDHM
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.
Solubility Information
DMSO: 20 mg/mL (47.12 mM), Sonication is recommended.
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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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:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent 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 DMSOTargetMol | reagent (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 DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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