| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
- Reactive oxygen species (ROS) generation regulatory targets [1]
- Glutathione (GSH) metabolism-related targets [1] |
|---|---|
| ln Vitro |
- Theaflavin-3'-gallate exhibited prooxidant activity in human erythrocytes and rat hepatocytes. In erythrocytes, it induced dose-dependent hemolysis: at 50 μM, hemolysis rate was 32 ± 3%; at 100 μM, it reached 78 ± 4% after 24 hours of incubation [1]
- It depleted intracellular glutathione (GSH) levels in hepatocytes: 100 μM Theaflavin-3'-gallate reduced GSH content by 65 ± 5% compared to the control group, accompanied by a 2.8 ± 0.3-fold increase in ROS production [1] - The compound showed concentration-dependent cytotoxicity to rat hepatocytes, with an IC50 value of 72.5 ± 4.1 μM (24-hour incubation). At 150 μM, cell viability was reduced to 22 ± 3% [1] - It induced apoptosis in hepatocytes, as evidenced by increased caspase-3 activity (1.9 ± 0.2-fold at 100 μM) and phosphatidylserine externalization (Annexin V-positive cells increased by 45 ± 4% at 100 μM) [1] - In erythrocytes, it promoted lipid peroxidation, with malondialdehyde (MDA) levels increased by 2.1 ± 0.2-fold at 100 μM [1] |
| Enzyme Assay |
- ROS detection assay: Rat hepatocytes were seeded in 96-well plates and treated with Theaflavin-3'-gallate (25, 50, 100, 150 μM) for 24 hours. Cells were loaded with a ROS-specific fluorescent probe, incubated for 30 minutes, and fluorescence intensity was measured at excitation/emission wavelengths of 488/525 nm to quantify ROS levels [1]
- GSH quantification assay: Hepatocytes were treated with the compound (50, 100 μM) for 24 hours, then lysed. The lysate was mixed with a GSH detection reagent, incubated at 37°C for 15 minutes, and absorbance was measured at 412 nm to determine GSH concentration [1] - Lipid peroxidation assay: Human erythrocytes were incubated with Theaflavin-3'-gallate (25, 50, 100 μM) for 24 hours. Erythrocyte lysate was mixed with thiobarbituric acid (TBA) reagent, heated at 95°C for 60 minutes, and MDA-TBA adduct absorbance was measured at 532 nm [1] |
| Cell Assay |
- Erythrocyte hemolysis assay: Human erythrocytes were suspended in buffer and incubated with Theaflavin-3'-gallate (10, 25, 50, 100 μM) for 24 hours. The mixture was centrifuged, and absorbance of the supernatant was measured at 540 nm to calculate hemolysis rate [1]
- Hepatocyte viability assay: Rat hepatocytes were seeded in 96-well plates (5×10³ cells/well) and treated with the compound (25, 50, 75, 100, 150 μM) for 24 hours. A colorimetric cell viability reagent was added, incubated for 4 hours, and absorbance was measured at 570 nm to calculate IC50 value [1] - Hepatocyte apoptosis assay: Hepatocytes were treated with Theaflavin-3'-gallate (50, 100 μM) for 24 hours. Cells were stained with Annexin V-FITC and propidium iodide, then analyzed by flow cytometry to count apoptotic cells. Caspase-3 activity was measured using a colorimetric assay with a specific substrate [1] |
| Toxicity/Toxicokinetics |
Theaflavins-3'-gallate exhibited concentration-dependent cytotoxicity in rat hepatocytes (IC50 = 72.5 ± 4.1 μM) and human erythrocytes (100 μM induces 78 ± 4% hemolysis) [1] - It leads to glutathione (GSH) depletion and excessive reactive oxygen species (ROS) production in hepatocytes, which is the key mechanism of its prooxidative toxicity [1]
|
| References | |
| Additional Infomation |
Theaflavins-3'-gallic acid ester is a natural polyphenol derived from black tea and belongs to the theaflavins family [1]. Its pro-oxidative mechanism involves the consumption of the intracellular antioxidant glutathione (GSH) and the promotion of reactive oxygen species (ROS) generation, which leads to oxidative stress, lipid peroxidation, and ultimately cell damage or apoptosis [1]. Compared with theaflavins-3'-gallic acid ester (another theaflavin from black tea), theaflavins-3'-gallic acid ester exhibits stronger pro-oxidative activity and cytotoxicity [1]. Its pro-oxidative properties suggest its potential application value in targeting oxidative stress-sensitive cells (such as cancer cells), but also suggest the need to carefully evaluate its toxicity to normal cells [1].
|
| Molecular Formula |
C36H32O15
|
|---|---|
| Molecular Weight |
704.63
|
| Exact Mass |
704.174
|
| CAS # |
28543-07-9
|
| Appearance |
Brown to reddish brown solid powder
|
| Density |
1.8±0.1 g/cm3
|
| Boiling Point |
1135.6±65.0 °C at 760 mmHg
|
| Flash Point |
361.0±27.8 °C
|
| Vapour Pressure |
0.0±0.3 mmHg at 25°C
|
| Index of Refraction |
1.836
|
| LogP |
4.61
|
| 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 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)
|
| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~69.77 mM)
|
|---|---|
| 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 | 1.4192 mL | 7.0959 mL | 14.1918 mL | |
| 5 mM | 0.2838 mL | 1.4192 mL | 2.8384 mL | |
| 10 mM | 0.1419 mL | 0.7096 mL | 1.4192 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
