| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg | |||
| 500mg | |||
| Other Sizes |
| Targets |
Not well characterized; potential targets include inflammatory pathways (NF-κB, COX-2), viral enzymes, and cancer-related pathways (PI3K/Akt, MAPK).
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|---|---|
| ln Vitro |
In a concentration- and time-dependent manner, arctigenin (0.01-1 μg/mL; 0.5-24 h) demonstrates preferential cytotoxicity to the PANC-1 cell line under nutrient-starved conditions [1]. In situations of nutrient deficiency, arctigenin (0.01-1 μg/mL; 0.5-24 h) inhibits the survival of several cancer cell lines (ASPC-1, BXPC-3, Alexander, and PSN-1 cells) [1]. In PANC-1 cells, arctigenin (0.1–1 μg/mL; 24 hours) totally prevents glucose deprivation-stimulated Akt phosphorylation [1]. With an IC50 of 2.9 μM, arctigenin (5–25 μM) exhibits strong in vitro antiviral activity against the influenza A virus[3].
In vitro, Arctigenin exhibits anti-inflammatory activity by inhibiting NF-κB activation and COX-2 expression. It shows antiviral activity against various viruses and anticancer activity against multiple cancer cell lines. Quantitative IC50 values vary depending on the cell line and assay; typical ranges are in the micromolar to sub-micromolar range. |
| ln Vivo |
Arctigenin (250 μg/mL; 0.2 mL; intraperitoneally administered 6 times per week for 9 weeks) suppresses the formation of PANC-1 tumors in nude mice [1]. ?Arctigenin (10 mg/kg; daily intraperitoneal injection for 30 days) alleviates the symptoms of experimental autoimmune encephalomyelitis (EAE) in mice [4].
In vivo, Arctigenin has shown anti-inflammatory, antiviral, and anticancer effects in animal models. It has been studied for its potential in treating influenza, hepatitis, and various cancers. Detailed dose-response data is available in specific studies but not summarized here. |
| Enzyme Assay |
No specific cell-free assay protocol is detailed for Arctigenin. For lignans, typical cell-free assays include enzyme inhibition assays (e.g., COX-2, LOX, viral protease) and antioxidant assays.
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| Cell Assay |
Cellular activity is assessed in various cell lines (inflammatory cells, virus-infected cells, cancer cells). Cells are treated with Arctigenin, and endpoints include cytokine production (ELISA), viral titer (plaque assay), cell viability (MTT), and signaling pathway analysis (Western blot).
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| Animal Protocol |
Animal/Disease Models: Female SPF/VAF BALB/cAn Ncrj-nu/nu (nude) mice were injected with PANC-1 cells [1]
Doses: 250 μg/mL, 0.2 mL Route of Administration: intraperitoneal (ip) injection 6 times a week for 9 weeks Experimental Results: Tumors shrink in weight and size. No significant weight loss was noted. In vivo efficacy is evaluated in animal models of disease (e.g., influenza-infected mice, tumor xenografts). Arctigenin is administered via oral gavage or intraperitoneal injection. Endpoints include survival, viral load, tumor volume, and biomarker analysis. |
| ADME/Pharmacokinetics |
Molecular weight: 372.41; molecular formula: C21H24O6. Solubility: soluble in DMSO, ethanol; poorly soluble in water. Storage: typical for lignans (desiccated, protected from light, -20°C).
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| Toxicity/Toxicokinetics |
No detailed toxicity data is publicly available. As a natural lignan, it is generally considered to have low toxicity, but standard toxicological studies would be required for drug development.
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| References |
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| Additional Infomation |
Arctigenin (-) is a lignan. Arctigenin has been reported in Saussurea salicifolia, Saussurea salicifolia, and other organisms for which data are available. See also: Lignans (subclasses of lignans); Burdock fruit (part); Burdock root (part)... See more...
Arctigenin is a research-grade compound, not approved for therapeutic use. It is primarily used for pharmacological research in inflammation, virology, and oncology. No FDA approval has been reported. Its mechanisms involve inhibition of NF-κB, COX-2, and viral enzymes. |
| Molecular Formula |
C21H24O6
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|---|---|
| Molecular Weight |
372.4117
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| Exact Mass |
372.157
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| CAS # |
7770-78-7
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| Related CAS # |
25488-59-9 (methyl ether); 26788-57-8 (mustard);
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| PubChem CID |
64981
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
567.0±45.0 °C at 760 mmHg
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| Melting Point |
100 °C
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| Flash Point |
198.8±22.2 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.576
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| LogP |
2.47
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
27
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| Complexity |
483
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| Defined Atom Stereocenter Count |
2
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| SMILES |
COC1=C(C=C(C=C1)C[C@H]2COC(=O)[C@@H]2CC3=CC(=C(C=C3)O)OC)OC
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| InChi Key |
NQWVSMVXKMHKTF-JKSUJKDBSA-N
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| InChi Code |
InChI=1S/C21H24O6/c1-24-18-7-5-13(11-20(18)26-3)8-15-12-27-21(23)16(15)9-14-4-6-17(22)19(10-14)25-2/h4-7,10-11,15-16,22H,8-9,12H2,1-3H3/t15-,16+/m0/s1
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| Chemical Name |
(3R,4R)-4-[(3,4-dimethoxyphenyl)methyl]-3-[(4-hydroxy-3-methoxyphenyl)methyl]oxolan-2-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 |
| 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 : ~100 mg/mL (~268.52 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.71 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 (6.71 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 25.0 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: ≥ 2.5 mg/mL (6.71 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 | 2.6852 mL | 13.4261 mL | 26.8521 mL | |
| 5 mM | 0.5370 mL | 2.6852 mL | 5.3704 mL | |
| 10 mM | 0.2685 mL | 1.3426 mL | 2.6852 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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