| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| Targets |
6-Demethoxytangeretin targets multiple signaling pathways and proteins. Its primary targets include anaplastic lymphoma kinase (ALK), p38 MAPK, ERK, JNK, JAK, STAT, and Akt. The compound modulates the MAPK/ERK pathway, the JAK/STAT signaling pathway, and the PI3K/Akt/mTOR pathway. It also affects interleukin-related signaling and immunology/inflammation pathways. By inhibiting ALK and MAPK phosphorylation, 6-Demethoxytangeretin suppresses the production and gene expression of interleukin-6 (IL-6) in human mast cells. Additionally, the compound facilitates CRE-mediated transcription, which is involved in learning and memory processes in hippocampal neurons. Its multi-target profile makes it a valuable tool for studying interconnected inflammatory and neurodegenerative signaling networks.
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| ln Vitro |
In vitro studies have demonstrated that 6-Demethoxytangeretin exerts potent anti-inflammatory and anti-allergic activities. At concentrations ranging from 0.8 to 20 μM, the compound inhibits the expression and production of IL-6 and other inflammatory factors in HMC-1 human mast cells stimulated with Phorbol 12-myristate 13-acetate (PMA) and Calcimycin. This inhibition is achieved through suppression of ALK and MAPK phosphorylation. The compound also facilitates CRE-mediated transcription in cultured hippocampal neurons, suggesting a role in learning and memory enhancement. Furthermore, 6-Demethoxytangeretin regulates signaling pathways associated with oxidative stress, apoptosis, and tumor growth inhibition. Its antioxidant properties contribute to its cytoprotective effects in various cell models.
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| ln Vivo |
In vivo activity data for 6-Demethoxytangeretin are limited, as the compound is primarily used in in vitro research settings. Based on its anti-inflammatory and neuroprotective properties observed in vitro, the compound may have potential therapeutic applications in inflammatory diseases and neurodegenerative disorders. However, specific published in vivo studies evaluating the efficacy and pharmacokinetics of 6-Demethoxytangeretin in animal models are not well documented. The compound's polymethoxyflavone structure suggests it may have reasonable oral bioavailability, as other PMFs such as tangeretin and nobiletin are known to be absorbed and metabolized in vivo.
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| Enzyme Assay |
In vitro non-cell enzyme/receptor binding assays for 6-Demethoxytangeretin typically involve kinase inhibition assays to evaluate its effects on ALK, MAPK, and other signaling kinases. These assays use purified recombinant kinases incubated with the compound and ATP in appropriate buffer systems, with kinase activity measured using radioactive or fluorescence-based detection methods. Binding affinity to target proteins can be assessed using surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC). Competitive binding assays may be employed to determine IC₅₀ values for specific kinase targets.
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| Cell Assay |
In vitro cell-based assays for 6-Demethoxytangeretin commonly use HMC-1 human mast cells or other relevant cell lines. Cells are cultured in appropriate media and stimulated with PMA and calcimycin to induce inflammatory responses. Following treatment with 6-Demethoxytangeretin at various concentrations (typically 0.8-20 μM for 1-6.5 hours), IL-6 and other inflammatory cytokine levels in the culture supernatant are measured by ELISA. Gene expression is analyzed by real-time quantitative PCR. Phosphorylation of ALK and MAPK proteins is assessed by Western blotting using phospho-specific antibodies. In neuronal studies, CRE-mediated transcription is evaluated using reporter gene assays in cultured hippocampal neurons.
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| Animal Protocol |
In vivo animal studies for 6-Demethoxytangeretin are not extensively documented. Based on standard protocols for evaluating flavonoid compounds, potential in vivo studies would involve oral administration of the compound to rodent models of inflammation (e.g., carrageenan-induced paw edema, LPS-induced inflammation) or neurodegenerative disease. Parameters assessed would include inflammatory cytokine levels in serum and tissues, histological examination, behavioral tests for cognitive function, and analysis of signaling pathway activation in target tissues. However, specific published protocols for this compound are limited.
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| ADME/Pharmacokinetics |
6-Demethoxytangeretin has a molecular weight of 342.34 g/mol and a molecular formula of C₁₉H₁₈O₆. It is soluble in DMSO at concentrations up to 12.5 mg/mL (36.51 mM) with ultrasonic and heating to 60°C. The compound should be stored as a powder at -20°C for up to three years or at 4°C protected from light. In solvent, it can be stored at -80°C for six months or at -20°C for one month. For in vivo formulations, a 10% DMSO in 90% corn oil solution can be prepared. Detailed pharmacokinetic parameters have not been extensively characterized.
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| Toxicity/Toxicokinetics |
The toxicity profile of 6-Demethoxytangeretin has not been comprehensively evaluated in published studies. As a naturally occurring citrus flavonoid, it is generally considered to have low toxicity, consistent with the safety profile of other polymethoxyflavones found in citrus fruits. The compound is classified as a research reagent and is not intended for human therapeutic use. Standard laboratory safety precautions should be followed when handling the compound. Comprehensive toxicological studies, including acute, subchronic, and chronic toxicity assessments, have not been reported in the literature.
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| References |
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| Additional Infomation |
6-Demethoxyhesperidin is an ether compound belonging to the flavonoid family. It has been reported to be found in citrus (Citrus reticulata), star anise (Citrus hassaku), and other organisms with relevant data. See also: orange peel (partial); sour orange (Citrus aurantium) peel (partial); tetramethylbaicalein (note moved here).
6-Demethoxytangeretin is a citrus flavonoid isolated from Citrus reticulata and Citrus depressa. It is also known by synonyms including 5,7,8-Trimethoxy-2-(4-methoxyphenyl)-4H-1-benzopyran-4-one. The compound exhibits multiple biological activities including anti-inflammatory, anti-allergic, anticancer, antioxidant, and neuroprotective effects. It is used as a research tool for studying ALK and MAPK signaling pathways, inflammation, and neurodegeneration. It is also a component of traditional Chinese medicinal herbs such as Hua Ju Hong (Citrus grandis) and Zhi Shi (Citrus aurantium). Not approved for clinical use; intended for research purposes only. |
| Molecular Formula |
C19H18O6
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| Molecular Weight |
342.3426
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| Exact Mass |
342.11
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| CAS # |
6601-66-7
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| PubChem CID |
629964
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| Appearance |
White to off-white solid powder
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| Density |
1.243±0.06 g/cm3
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| Boiling Point |
536.9±50.0 °C at 760 mmHg
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| Melting Point |
216-217 ºC
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| Flash Point |
237.5±30.2 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.575
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| LogP |
3.06
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
25
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| Complexity |
496
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
DDGJUTBQQURRGE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H18O6/c1-21-12-7-5-11(6-8-12)14-9-13(20)17-15(22-2)10-16(23-3)18(24-4)19(17)25-14/h5-10H,1-4H3
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| Chemical Name |
5,7,8-trimethoxy-2-(4-methoxyphenyl)chromen-4-one
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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 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)
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| Solubility (In Vitro) |
DMSO : ~12.5 mg/mL (~36.51 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (3.65 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 12.5 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 | 2.9211 mL | 14.6054 mL | 29.2107 mL | |
| 5 mM | 0.5842 mL | 2.9211 mL | 5.8421 mL | |
| 10 mM | 0.2921 mL | 1.4605 mL | 2.9211 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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