| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Eupafolin targets multiple pathways involved in inflammation and oxidative stress. It inhibits iron-dependent lipid peroxidation, reducing oxidative damage to cellular membranes. Eupafolin also inhibits the production of pro-inflammatory cytokines such as IL-6 in ARPE-19 cells. Its anti-inflammatory activity is mediated through the suppression of inflammatory signaling pathways, although the exact molecular targets have not been fully elucidated.
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| ln Vitro |
The production of IL-6, IL-8, and MCP-1 is dose-dependently inhibited by a pretreatment of nereptin, with IC50 values of 4.43, 3.42, and 4.17 μM, respectively [1]. The expression of IL-1β-induced cytokine (IL-6, IL-8, and MCP-1) mRNA levels in ARPE-19 cells is inhibited by nereptin (2.5–10 μM; 25 hours) treatment [1]. Nepetin treatment (2.5-10 μM; 1.5 h; ARPE-19 cells) dose-dependently reduced p65's nuclear translocation and the phosphorylation of IKKα/β and IκBα. In activated ARPE-19 cells, napetin lowers the amounts of phosphorylated ERK1/2, JNK, and p38 MAPK [1].
In vitro, eupafolin inhibits iron-dependent lipid peroxidation in a cell-free assay with an IC50 of 7.9 μM. It inhibits IL-6 production in ARPE-19 cells. Eupafolin exhibits potent anti-inflammatory activity. Its ability to inhibit lipid peroxidation and cytokine production has been confirmed in various cell-based assays. As a flavonoid, eupafolin also exhibits antioxidant activity. |
| ln Vivo |
In vivo, eupafolin has been studied for its anti-inflammatory effects, although specific in vivo efficacy data in animal models are not extensively detailed in the available literature. Its ability to inhibit IL-6 production and lipid peroxidation suggests potential therapeutic applications in inflammatory diseases. Further studies would be required to evaluate its therapeutic potential.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for eupafolin are not typical because it acts through multiple mechanisms rather than a single enzyme or receptor. However, its ability to inhibit lipid peroxidation can be assessed using cell-free assays measuring malondialdehyde (MDA) or other lipid peroxidation products. Its antioxidant activity can be assessed using DPPH or ABTS radical scavenging assays.
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| Cell Assay |
RT-PCR[1]
Cell Types: ARPE-19 Cell Tested Concentrations: 2.5 μM, 5 μM, 10 μM Incubation Duration: 25 hrs (hours) Experimental Results: Inhibition of the mRNA expression of IL-6, IL-8 and MCP-1 in ARPE-19 cells . Western Blot Analysis[1] Cell Types: ARPE-19 Cell Tested Concentrations: 2.5 μM, 5 μM, 10 μM Incubation Duration: 1.5 hrs (hours) Experimental Results: Dose-dependent inhibition of IKKα/β and IκBα phosphorylation and p65 nuclear translocation. Reduces the levels of phosphorylated ERK1/2, JNK and p38 MAPK in activated ARPE-19 cells. In vitro cellular assays for eupafolin are performed using ARPE-19 cells or other cell types. Cells are treated with varying concentrations of eupafolin and stimulated with inflammatory agents such as IL-1β or TNF-α. IL-6 production is measured by ELISA. Cell viability is evaluated using MTT assays to ensure that the observed anti-inflammatory effects are not due to cytotoxicity. Lipid peroxidation is measured using fluorescent probes. |
| Animal Protocol |
In vivo animal experiments for eupafolin have not been extensively documented in the available literature. However, to evaluate its anti-inflammatory effects, animal models of inflammation such as carrageenan-induced paw edema or LPS-induced endotoxemia could be used. Detailed protocols are not available in the published literature.
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| ADME/Pharmacokinetics |
Metabolism / Metabolites
Known human metabolites of 6-methoxyluteolin include (2S,3S,4S,5R)-6-[2-(3,4-dihydroxyphenyl)-5-hydroxy-6-methoxy-4-oxochromen-7-yl]oxy-3,4,5-trihydroxyoxacyclohexane-2-carboxylic acid. Eupafolin has a molecular weight of 316.27 g/mol and a molecular formula of C16H12O7. It is a natural flavonoid isolated from Eupatorium ballotaefolium HBK. The compound is also known as Nepetin and 6-Methoxyluteolin. It is soluble in methanol and slightly soluble in water. Detailed pharmacokinetic parameters have not been extensively reported. |
| Toxicity/Toxicokinetics |
The toxicological profile of eupafolin has not been extensively characterized. As a natural flavonoid, eupafolin is generally considered to have a favorable safety profile. No significant toxicity has been reported in the available literature. However, comprehensive toxicology studies would be necessary to fully assess its safety for clinical development.
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| References | |
| Additional Infomation |
It has been reported that 6-methoxyluteolin is found in sage (Salvia plebeia), coreopsis (Coreopsis lanceolata), and several other organisms with available data. See also: Arnica flowers (partial).
Eupafolin is a natural flavonoid with potent anti-inflammatory activities. It is also known as Nepetin and 6-Methoxyluteolin. Eupafolin inhibits iron-dependent lipid peroxidation with an IC50 of 7.9 μM. It inhibits IL-6 production in ARPE-19 cells. Eupafolin is a research compound with potential applications in inflammatory diseases. |
| Molecular Formula |
C16H12O7
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| Molecular Weight |
316.265
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| Exact Mass |
316.058
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| CAS # |
520-11-6
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| PubChem CID |
5317284
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| Appearance |
White to yellow solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
659.1±55.0 °C at 760 mmHg
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| Melting Point |
267ºC
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| Flash Point |
250.9±25.0 °C
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| Vapour Pressure |
0.0±2.1 mmHg at 25°C
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| Index of Refraction |
1.727
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| LogP |
1.89
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
23
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| Complexity |
491
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
FHHSEFRSDKWJKJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H12O7/c1-22-16-11(20)6-13-14(15(16)21)10(19)5-12(23-13)7-2-3-8(17)9(18)4-7/h2-6,17-18,20-21H,1H3
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| Chemical Name |
2-(3,4-dihydroxyphenyl)-5,7-dihydroxy-6-methoxychromen-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: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~125 mg/mL (~395.24 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.58 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1619 mL | 15.8093 mL | 31.6186 mL | |
| 5 mM | 0.6324 mL | 3.1619 mL | 6.3237 mL | |
| 10 mM | 0.3162 mL | 1.5809 mL | 3.1619 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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