| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| 1g |
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| Targets |
Ethyl gallate targets multiple pathways involved in cancer progression, inflammation, and oxidative stress. It inhibits the mRNA levels of MMP-9 and MMP-2, phosphorylation of Akt, and protein expression of NF-κB. It suppresses proliferation and invasion in human breast cancer cells by modulating the PI3K/Akt pathway, inhibiting downstream targets such as NF-κB p-65, Bcl-2/Bax, and MMP-2/MMP-9. It activates the death receptor-dependent apoptotic pathway, increasing expression of caspases-8, -9, and -3. It also inhibits hydrogen peroxide signaling. Estrogenic activity has been reported.
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| ln Vitro |
Hydrogen peroxide is scavenged by the non-flavonoid phenolic compound ethyl gallate. Following a 24- or 48-hour ethyl gallate treatment, HL-60 cells displayed morphological alterations that included the production of apoptotic bodies and a shrinking of the cell membrane. In line with these outcomes, ethyl gallate treatment caused time- and dose-dependent reductions in cell viability, suggesting that ethyl gallate is cytotoxic to HL-60 cells. The percentage of sub-G1 phase cells rose in response to ethyl gallate treatment in a concentration- and time-dependent manner. The percentage of cells in sub-G1 phase rose from 2.9% at baseline to 26.5% or 52.6% after treatment with 50 μM or 75 μM ethyl gallate for 24 or 48 hours, respectively. Research has revealed that ethyl gallate was used to treat HL-60 cells. Following a 24-hour treatment with 75 μM ethyl gallate, Bcl-2 expression decreased while Bax and truncated Bid (tBid) expression rose [1].
In vitro, Ethyl gallate obviously decreases cell proliferation in MDA-MB-231 and MCF-7 cells in a dose- and time-dependent manner. It exhibits cytotoxicity in a dose-dependent manner. Ethyl gallate can inhibit the abilities of invasion of breast cancer in vitro by inhibiting the mRNA levels of MMP-9/MMP-2, phosphorylation of Akt, and protein expression of NF-κB. After treatment for 24 h or 48 h with Ethyl gallate, HL-60 cells show changes in morphology, including shrinkage of the cell. It induces apoptosis in HL-60 cells by promoting the expression of caspases-8, -9, -3, apoptosis-inducing factor, and endonuclease G. It inhibits hydrogen peroxide signaling. |
| ln Vivo |
Rats given ethyl gallate equivalents of Nile tilapia leaf extract and rats fed ethyl gallate alone did not differ significantly in serum total protein, albumin, globulin, and glucose. Nonetheless, there were notable variations in total bilirubin levels between rats given 500 mg/kg body weight (ethyl gallate equivalent to 10 mg/kg, 0.34±0.01 mg/dL) and Nile tilapia (L.) leaf extract given 500 mg/kg body weight. received 10 mg/kg body weight (0.26 ± 0.01 mg/dL) of ethyl gallate. Between the groups given 10 and 20 mg/kg of ethyl gallate and 500 and 1000 mg/kg body weight of Nile tilapia leaf extract (26.52±1.23 and 30.05±1.38 U/L), there was a significant presence of ALT. The distinction. Twenty.50±0.94 and twenty-four.67±1.13 U/L)[2].
In vivo, Ethyl gallate may represent an alternative class of vasopressors for use in septic shock. It has been studied for its potential use in hormone replacement therapy due to its estrogenic activity. As a hydrogen peroxide scavenger and antioxidant, it may have protective effects against oxidative stress-related conditions. However, detailed in vivo efficacy studies, including pharmacokinetic and pharmacodynamic parameters, are limited in the available literature. Further research is needed to fully characterize its in vivo activity and therapeutic potential. |
| Enzyme Assay |
For in vitro cell-free assays, the antioxidant activity of Ethyl gallate can be measured using hydrogen peroxide scavenging assays. Its inhibitory effects on MMP-2/MMP-9 can be assessed using gelatin zymography or fluorogenic substrate assays. NF-κB activity can be measured using DNA-binding ELISA or reporter gene assays. Caspase activity can be quantified using fluorogenic substrates (e.g., DEVD-AFC for caspase-3, IETD-AFC for caspase-8, LEHD-AFC for caspase-9). The PI3K/Akt pathway can be studied using kinase activity assays or by measuring phosphorylation levels.
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| Cell Assay |
For in vitro cellular assays, the anticancer activity of Ethyl gallate is assessed in breast cancer cell lines such as MDA-MB-231 and MCF-7. Cells are treated with various concentrations of Ethyl gallate for 24-48 hours. Cell viability is measured using MTT or SRB assays. Apoptosis is assessed by morphological changes, flow cytometry (Annexin V/PI staining), and caspase activity assays. MMP-2/MMP-9 mRNA levels are measured by qPCR, and protein expression of NF-κB, Akt phosphorylation, and Bcl-2/Bax are assessed by Western blot.
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| Animal Protocol |
For in vivo studies, Ethyl gallate could be administered orally or intravenously in animal models of cancer, septic shock, or hormone-related conditions. In cancer models, endpoints include tumor volume measurement, metastasis assessment, and survival analysis. In septic shock models, its vasopressor effects could be evaluated by measuring blood pressure and inflammatory markers. Its estrogenic activity could be studied in ovariectomized animal models.
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| ADME/Pharmacokinetics |
Ethyl gallate (CAS 831-61-8) has a molecular formula of C9H10O5 and a molecular weight of 198.17 g/mol. It is also known as Phyllemblin and Nipagallin A. Appearance: typically a powder. Solubility: DMSO 36 mg/mL (181.66 mM). For in vivo formulation: 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline, solubility 2 mg/mL (10.09 mM). Density: 1.424 g/cm3. Storage: powder at -20°C for 3 years; in solvent at -80°C for 1 year. Purity: 99.96%.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is publicly available. As a natural phenolic compound, it is generally considered to have low toxicity, but standard toxicological studies would be required for drug development. It could be used as a potential antioxidant with safe therapeutic application in cancer chemotherapy. In vitro cytotoxicity assays in various cell lines are typically performed alongside efficacy studies to confirm that observed effects are not due to a general reduction in cell viability.
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| References |
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| Additional Infomation |
Ethyl gallate is a gallic acid ester formed by the condensation of gallic acid and ethanol. It is a plant metabolite. Ethyl gallate has been reported in Phyllanthus sellowianus, Acer truncatum, and other organisms with relevant data.
Ethyl gallate is a research-grade compound and is not approved for therapeutic use. It serves primarily as a pharmacological tool for studying apoptosis, cancer cell biology, and oxidative stress. Its mechanism of action involves the activation of the death receptor-dependent apoptotic pathway, increasing expression of caspases-8, -9, and -3. It suppresses proliferation and invasion in human breast cancer cells by modulating the PI3K/Akt pathway. It exhibits estrogenic activity with potential use in hormone replacement therapy. No clinical trials have been reported. |
| Molecular Formula |
C9H10O5
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|---|---|
| Molecular Weight |
198.1727
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| Exact Mass |
198.052
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| CAS # |
831-61-8
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| PubChem CID |
13250
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
447.3±40.0 °C at 760 mmHg
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| Melting Point |
149-153 °C
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| Flash Point |
185.0±20.8 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.611
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| LogP |
2.07
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
14
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| Complexity |
193
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
VFPFQHQNJCMNBZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C9H10O5/c1-2-14-9(13)5-3-6(10)8(12)7(11)4-5/h3-4,10-12H,2H2,1H3
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| Chemical Name |
ethyl 3,4,5-trihydroxybenzoate
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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 (~504.62 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (12.62 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 (12.62 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 (12.62 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 | 5.0462 mL | 25.2309 mL | 50.4617 mL | |
| 5 mM | 1.0092 mL | 5.0462 mL | 10.0923 mL | |
| 10 mM | 0.5046 mL | 2.5231 mL | 5.0462 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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