| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
EC50: 3.417 μM (Dopamine transporter)[1]
5,7-Dimethoxyluteolin acts as a dopamine transporter (DAT) activator. It activates DAT with an EC50 of 3.417 μM. Unlike DAT inhibitors that block dopamine uptake, this compound enhances DAT function, representing a distinct mechanism of modulating dopaminergic signaling. |
|---|---|
| ln Vitro |
In cell-free systems, 5,7-Dimethoxyluteolin demonstrates activity at the dopamine transporter with an EC50 of 3.417 μM. The compound's flavonoid structure enables interactions with multiple biological targets, contributing to its antioxidant and anti-inflammatory activities. In cellular assays, 5,7-Dimethoxyluteolin activates dopamine transporter function with an EC50 of 3.417 μM. The compound enhances DAT-mediated dopamine uptake in cells expressing the transporter. Additionally, it exhibits antioxidant effects in cell culture models, reducing oxidative stress markers. Its anti-inflammatory activity has been demonstrated in various cellular systems.
|
| ln Vivo |
In vivo studies on 5,7-Dimethoxyluteolin are limited. As a naturally occurring flavonoid, it may contribute to the pharmacological effects of plant extracts containing this compound. The compound's DAT activator properties suggest potential effects on dopaminergic signaling in vivo, but detailed animal studies have not been extensively reported.
|
| Enzyme Assay |
Cell-free receptor binding or enzyme assays for 5,7-Dimethoxyluteolin typically involve testing its activity at the dopamine transporter using membrane preparations. Radioligand binding studies or functional uptake assays are performed to determine its EC50 for DAT activation. Antioxidant activity is assessed using cell-free systems such as DPPH radical scavenging assays.
|
| Cell Assay |
Cellular assays for 5,7-Dimethoxyluteolin are conducted using cells expressing the dopamine transporter. Cells are treated with various concentrations of the compound, and dopamine uptake is measured to determine DAT activation. Anti-inflammatory activity is assessed in macrophage or other immune cell models by measuring cytokine production or NF-κB activation following compound treatment.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of 5,7-Dimethoxyluteolin have not been extensively characterized. As a flavonoid, it is likely subject to extensive metabolism via phase II conjugation reactions. Oral bioavailability may be limited due to poor aqueous solubility and first-pass metabolism, consistent with other flavonoid compounds. Detailed PK parameters remain to be established.
|
| Toxicity/Toxicokinetics |
Toxicity data for 5,7-Dimethoxyluteolin are limited. As a naturally occurring compound found in dietary plants, it is generally considered to have low toxicity. However, comprehensive toxicological studies have not been performed. The compound's antioxidant properties may provide protective effects against oxidative damage, while high concentrations could potentially have pro-oxidant effects.
|
| References | |
| Additional Infomation |
5,7-Dimethoxyluteolin is a research compound with potential therapeutic applications in neurodegenerative diseases, inflammation, and cancer. Its unique DAT activator mechanism distinguishes it from typical dopamine transporter inhibitors. The compound has not progressed to clinical trials. It is available as a high-purity research standard for pharmacological studies.
|
| Molecular Formula |
C17H14O6
|
|---|---|
| Molecular Weight |
314.29
|
| Exact Mass |
314.079
|
| CAS # |
90363-40-9
|
| PubChem CID |
13964548
|
| Appearance |
White to light yellow solid powder
|
| LogP |
2.888
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
23
|
| Complexity |
476
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
COC1=CC2=C(C(=C1)OC)C(=O)C=C(O2)C3=CC(=C(C=C3)O)O
|
| InChi Key |
NKGJZNRUAGQIRY-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C17H14O6/c1-21-10-6-15(22-2)17-13(20)8-14(23-16(17)7-10)9-3-4-11(18)12(19)5-9/h3-8,18-19H,1-2H3
|
| Chemical Name |
2-(3,4-dihydroxyphenyl)-5,7-dimethoxychromen-4-one
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: 100 mg/mL (318.18 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.95 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 25.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1818 mL | 15.9089 mL | 31.8177 mL | |
| 5 mM | 0.6364 mL | 3.1818 mL | 6.3635 mL | |
| 10 mM | 0.3182 mL | 1.5909 mL | 3.1818 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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