| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| ln Vitro |
Theaflavin-3-gallate exhibits prooxidant properties in vitro, inducing reactive oxygen species (ROS) generation in a concentration-dependent manner (10-100 μM) in HepG2, HeLa, and Caco-2 cells[1]
Theaflavin-3-gallate depletes intracellular glutathione (GSH) levels in HepG2 cells, with a 40% reduction observed at 50 μM after 24 hours of incubation; this GSH depletion is associated with enhanced lipid peroxidation, as indicated by increased thiobarbituric acid reactive substances (TBARS) levels[1] Theaflavin-3-gallate exerts cytotoxic effects on cancer cell lines (HepG2, HeLa, Caco-2) with IC₅₀ values ranging from 45 to 68 μM (24-hour incubation), and the cytotoxicity is iron-dependent—chelating iron ions abolishes its prooxidant and cytotoxic effects[1] Theaflavin-3-gallate induces apoptotic cell death in HepG2 cells, characterized by DNA fragmentation, increased caspase-3 activity, and phosphatidylserine externalization detected via Annexin V-FITC staining[1] |
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| Enzyme Assay |
For ROS generation assay: Culture target cells in 96-well plates; load cells with DCFH-DA probe (10 μM) for 30 minutes at 37°C; treat cells with Theaflavin-3-gallate (10-100 μM) for 24 hours; measure fluorescence intensity using a microplate reader (excitation 485 nm, emission 535 nm) to quantify ROS levels[1]
For GSH detection assay: Lyse HepG2 cells treated with Theaflavin-3-gallate (10-80 μM) for 24 hours; add GSH detection reagent to the cell lysate, incubate at room temperature for 15 minutes; measure absorbance at 405 nm to determine GSH concentration[1] For lipid peroxidation assay: Collect cells treated with Theaflavin-3-gallate (30-100 μM) for 48 hours; homogenize cells and mix with TBARS reagent; heat the mixture at 95°C for 60 minutes; cool to room temperature and measure absorbance at 532 nm to quantify TBARS levels[1] |
| Cell Assay |
For cytotoxicity assay: Seed HepG2, HeLa, and Caco-2 cells in 96-well plates (5×10³ cells/well); treat cells with Theaflavin-3-gallate (10-100 μM) for 24-72 hours; add MTT reagent and incubate for 4 hours; dissolve formazan crystals with DMSO; measure absorbance at 570 nm to calculate cell viability and IC₅₀ values[1]
For iron-dependent prooxidant assay: Divide HepG2 cells into two groups; pre-treat one group with iron chelator (100 μM) for 1 hour, then treat both groups with Theaflavin-3-gallate (50 μM) for 24 hours; measure ROS levels via DCFH-DA staining and cell viability via MTT assay to compare the effects with and without iron chelation[1] For apoptosis assay: Treat HepG2 cells with Theaflavin-3-gallate (40-80 μM) for 48 hours; isolate genomic DNA and analyze fragmentation via agarose gel electrophoresis; detect caspase-3 activity using a colorimetric assay kit; assess phosphatidylserine externalization via Annexin V-FITC/PI double-staining flow cytometry[1] |
| Toxicity/Toxicokinetics |
Theaflavins-3-gallate exhibit selective cytotoxicity against cancer cell lines (HepG2, HeLa, Caco-2) and have extremely low cytotoxicity against normal human fibroblasts (IC₅₀ > 100 μM after 24 hours) [1]. The pro-oxidative and cytotoxic effects of theaflavins-3-gallate are strictly dependent on iron and require the presence of transition metal ions to mediate ROS production and cell damage [1].
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| References | |
| Additional Infomation |
Theaflavin-3-gallate is a natural polyphenol belonging to the theaflavins family. It is mainly found in black tea (Camellia sinensis) and is a product of catechin oxidation during fermentation [1]. Its pro-oxidation mechanism involves redox cycles with transition metal ions (such as iron), leading to the generation of reactive oxygen species (ROS), thereby disrupting intracellular redox homeostasis (glutathione depletion, lipid peroxidation) and inducing apoptosis [1]. Unlike many other tea polyphenols with antioxidant properties, theaflavin-3-gallate mainly exerts its biological effects through pro-oxidation activity, which contributes to its cytotoxicity against cancer cells [1].
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| Molecular Formula |
C₃₆H₂₈O₁₆
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|---|---|
| Molecular Weight |
716.60
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| Exact Mass |
716.137
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| CAS # |
30462-34-1
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| Appearance |
Brown to reddish brown solid powder
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| Density |
1.8±0.1 g/cm3
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| Boiling Point |
1202.8±65.0 °C at 760 mmHg
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| Flash Point |
382.0±27.8 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.830
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| LogP |
2.45
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| Synonyms |
TF2A Theaflavin Monogallate A Theaflavin-3-gallate
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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 : ~50 mg/mL (~69.77 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.49 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.  (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3955 mL | 6.9774 mL | 13.9548 mL | |
| 5 mM | 0.2791 mL | 1.3955 mL | 2.7910 mL | |
| 10 mM | 0.1395 mL | 0.6977 mL | 1.3955 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.