| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
| Targets |
5,6,7-Trimethoxyflavone is a p38 MAPK inhibitor that exerts significant anti-inflammatory effects. By interfering with the p38 MAPK signaling pathway, the compound modulates the production of pro-inflammatory cytokines and inflammatory mediators. The p38 MAPK pathway is a key signaling cascade involved in the cellular response to stress, inflammation, and apoptosis. Inhibition of this pathway by 5,6,7-Trimethoxyflavone contributes to its anti-inflammatory and potential therapeutic effects in various inflammation-related diseases and tumor models. As a flavonoid, the compound also exhibits antioxidant activity by scavenging reactive oxygen species (ROS) and reducing oxidative stress. Its multiple mechanisms of action make it a compound of interest in the study of inflammatory diseases and cancer.
|
|---|---|
| ln Vitro |
In vitro, 5,6,7-Trimethoxyflavone demonstrates significant anti-inflammatory activity by inhibiting p38 MAPK signaling. It reduces the production of pro-inflammatory cytokines such as TNF-α, IL-1β, and IL-6 in activated immune cells. The compound's antioxidant activity is demonstrated by its ability to scavenge free radicals and reduce oxidative stress markers in cell culture models. Its anticancer properties have been evaluated in various cancer cell lines, where it inhibits cell proliferation and induces apoptosis. The compound has shown therapeutic potential in a variety of inflammation-related diseases and tumor models. Its effects on cell signaling pathways, including MAPK and NF-κB, have been characterized using Western blotting and reporter gene assays.
|
| ln Vivo |
In vivo, 5,6,7-Trimethoxyflavone has been studied for its anti-inflammatory and anticancer effects in animal models. Its inhibition of p38 MAPK signaling contributes to its therapeutic potential in inflammation-related diseases. The compound has been evaluated in models of acute and chronic inflammation, where it reduces inflammatory markers and tissue damage. Its anticancer activity has been assessed in xenograft models, where it inhibits tumor growth. The compound's antioxidant properties may also contribute to its protective effects in models of oxidative stress-related diseases. However, detailed in vivo efficacy data for 5,6,7-Trimethoxyflavone are limited in the public literature.
|
| Enzyme Assay |
For in vitro enzyme assays, 5,6,7-Trimethoxyflavone is evaluated for its ability to inhibit p38 MAPK activity. The kinase assay is performed using purified p38 MAPK enzyme and a suitable peptide substrate in the presence of ATP. The compound is incubated with the enzyme at various concentrations, and the phosphorylation of the substrate is measured using radioactive (³³P-ATP) or fluorescence-based detection methods. The IC₅₀ for p38 MAPK inhibition is determined from concentration-response curves. For antioxidant activity, cell-free assays such as DPPH radical scavenging, ABTS radical scavenging, and ferric reducing antioxidant power (FRAP) assays are used to measure the compound's ability to neutralize free radicals.
|
| Cell Assay |
For in vitro cell-based assays, immune cells (e.g., macrophages, monocytes) or cancer cell lines are cultured in appropriate media and treated with 5,6,7-Trimethoxyflavone at various concentrations (typically 1-100 μM). For anti-inflammatory studies, cells are stimulated with lipopolysaccharide (LPS) or other inflammatory stimuli in the presence of the compound. Pro-inflammatory cytokine production (TNF-α, IL-1β, IL-6) is measured by ELISA or qPCR. p38 MAPK phosphorylation is assessed by Western blotting. For anticancer studies, cell viability is measured by MTT or CCK-8 assays, apoptosis is assessed by Annexin V staining, and cell cycle distribution is analyzed by flow cytometry.
|
| Animal Protocol |
For in vivo animal studies, 5,6,7-Trimethoxyflavone is typically administered orally or intraperitoneally in rodent models. In models of inflammation (e.g., carrageenan-induced paw edema, LPS-induced endotoxemia), the compound is administered prior to or following the inflammatory insult, and inflammatory markers (cytokine levels, edema, tissue damage) are assessed. In cancer models, tumor-bearing mice are treated with the compound, and tumor volume and weight are measured. The compound's effects on oxidative stress markers (MDA, SOD, GSH) are evaluated in various tissues. Pharmacokinetic and toxicological studies may also be performed.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of 5,6,7-Trimethoxyflavone are not extensively characterized in the literature. As a small lipophilic flavonoid, the compound is expected to have reasonable oral bioavailability. Polymethoxyflavones are known to be metabolized in the liver by cytochrome P450 enzymes, and their metabolites may contribute to their biological activities. The compound's distribution to various tissues, including the brain, has not been extensively studied. Detailed parameters such as Cmax, Tmax, half-life, and bioavailability would require dedicated pharmacokinetic studies.
|
| Toxicity/Toxicokinetics |
Specific toxicity data for 5,6,7-Trimethoxyflavone are limited. Flavonoids are generally considered to have a favorable safety profile, and 5,6,7-Trimethoxyflavone is no exception. No significant adverse effects have been reported at research doses. However, as with any research chemical, standard safety precautions should be observed when handling the compound. Comprehensive toxicological studies, including repeated-dose toxicity, genotoxicity, and reproductive toxicity assessments, have not been published.
|
| References | |
| Additional Infomation |
5,6,7-Trimethoxyflavonoids are 5,6,7-trimethyl ether derivatives of baicalin. They have been isolated from Callicarpa japonica and have been shown to possess antiviral activity. They are both a plant metabolite and an anti-HSV-1 drug. Their function is related to baicalin. 5,6,7-Trimethoxyflavonoids have been reported to exist in Callicarpa japonica, Friesodielsia velutina, and other organisms with relevant data.
5,6,7-Trimethoxyflavone is a research compound with no clinical trial or regulatory approval status. It is a naturally occurring polymethoxyflavone found in citrus and other plants. The compound is used primarily as a reference standard and in pharmacological studies of anti-inflammatory, antioxidant, and anticancer activities. Its role as a p38 MAPK inhibitor makes it a valuable tool for studying inflammatory signaling pathways. The compound's structural similarity to baicalein, a well-studied flavonoid with multiple biological activities, makes it of interest for structure-activity relationship studies. It is commercially available from chemical suppliers for research purposes only. |
| Molecular Formula |
C18H16O5
|
|---|---|
| Molecular Weight |
312.31664
|
| Exact Mass |
312.1
|
| CAS # |
973-67-1
|
| PubChem CID |
442583
|
| Appearance |
White to light yellow solid powder
|
| Density |
1.242g/cm3
|
| Boiling Point |
497.4ºC at 760 mmHg
|
| Melting Point |
165-167°C
|
| Flash Point |
221.3ºC
|
| Index of Refraction |
1.585
|
| LogP |
3.485
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
23
|
| Complexity |
454
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
HJNJAUYFFFOFBW-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C18H16O5/c1-20-15-10-14-16(18(22-3)17(15)21-2)12(19)9-13(23-14)11-7-5-4-6-8-11/h4-10H,1-3H3
|
| Chemical Name |
5,6,7-trimethoxy-2-phenylchromen-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 |
| 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 : ~33.33 mg/mL (~106.72 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.00 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 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.00 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2018 mL | 16.0092 mL | 32.0184 mL | |
| 5 mM | 0.6404 mL | 3.2018 mL | 6.4037 mL | |
| 10 mM | 0.3202 mL | 1.6009 mL | 3.2018 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
