| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
IC50: 20.9 μM (GPR56)[1]; GPR114[1]
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|---|---|
| ln Vitro |
[35S]GTPηS is added to start assays, and rates of aGPCR-stimulated G protein activation ([35S]GTPηS binding to Gα) are measured with and without the presence of additional compounds. To differing degrees, GPR56 7TM-stimulated G13 GTPγS binding kinetics are inhibited by dihydromunduletone (DHM). With a reduction in GPR56 7TM activated G13 >75% (from 0.18 to 0.04 minutes−1), dihydromunduletone is the best inhibitory compound[1]. The rate of GPR114 7TM-stimulated Gs activity is also significantly inhibited at a concentration of Dihydromunduletone (DHM) that maximally inhibits GPR56 (50 μM). Dihydromunduletone (50 μM) does not prevent GPR110 stimulation of Gq GTPηS binding when it is applied to the GPR110 7TM[1]. Dihydromunduletone is incubated at escalating concentrations in cells transfected with GPR56 A386M 7TM. SRE-luciferase activity is assessed after the addition of P7 peptide agonist. In a concentration-dependent manner, dihydromunduletone inhibits the P7 peptide-induced luciferase activity. Additionally, cells are exposed to a fixed concentration of 3 µM dihydromunduletone before being stimulated with progressively higher concentrations of P7 peptide agonist. At every concentration, P7 peptide activation is blunted by dihydromunduletone treatment. As a result, in isolated membranes and HEK293T cell-based experiments, dihydromunduletone opposes synthetic-peptide agonist and tethered-peptide agonist-mediated aGPCR activation, but it does not impede basal receptor signaling[1].
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| References | |
| Additional Infomation |
1-(3,7-dihydroxy-2,2-dimethyl-3,4-dihydro-2H-1-benzopyran-6-yl)-2-(5-methoxy-2,2-dimethyl-1-benzopyran-6-yl)ethanone is a stilbenoid.
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| Molecular Formula |
C25H28O6
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|---|---|
| Molecular Weight |
424.486227989197
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| Exact Mass |
424.188
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| CAS # |
674786-20-0
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| PubChem CID |
3492326
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
4.3
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
31
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| Complexity |
700
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
RMVZECFNOTWEKD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H28O6/c1-24(2)9-8-16-20(30-24)7-6-14(23(16)29-5)11-18(26)17-10-15-12-22(28)25(3,4)31-21(15)13-19(17)27/h6-10,13,22,27-28H,11-12H2,1-5H3
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| Chemical Name |
1-(3,7-dihydroxy-2,2-dimethyl-3,4-dihydrochromen-6-yl)-2-(5-methoxy-2,2-dimethylchromen-6-yl)ethanone
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 250 mg/mL (588.94 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.90 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.90 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.90 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3558 mL | 11.7788 mL | 23.5577 mL | |
| 5 mM | 0.4712 mL | 2.3558 mL | 4.7115 mL | |
| 10 mM | 0.2356 mL | 1.1779 mL | 2.3558 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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