| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
| Targets |
EGCG Octaacetate targets multiple pathways including PI3K/Akt/NF-κB signaling, p65 acetylation, and the 20S proteasome. It downregulates PI3K/Akt/NF-κB phosphorylation and p65 acetylation to decrease pro-inflammatory mediator levels. It also inhibits the chymotrypsin-like activity of the 20S proteasome.
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|---|---|
| ln Vitro |
EGCG Octaacetate inhibits the chymotrypsin-like activity of the 20S proteasome at 50 µM with an inhibition rate of less than 20%. It exhibits antiviral properties against Influenza A/PR8/34(H1N1) with an EC50 of 8490 nM. It shows antiproliferative effects against human MDA-MB-231 cells, achieving 42% inhibition at 25 µM in cells with high COMT activity, enhanced to 89% in the presence of a COMT inhibitor. It induces AMPKα phosphorylation (3.9-fold change) at 20 µM after 3 hours.
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| ln Vivo |
EGCG Octaacetate reduces colitis-driven colon cancer in mice by downregulating PI3K/Akt/NF-κB phosphorylation and p65 acetylation. It has potential antibacterial activity against both Gram-positive and Gram-negative bacteria. The prodrug enhances the stability and bioavailability of EGCG in vivo, improving its therapeutic efficacy.
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| Enzyme Assay |
For proteasome inhibition assays, the 20S proteasome is incubated with a fluorogenic substrate (e.g., Suc-LLVY-AMC) and varying concentrations of EGCG Octaacetate. Proteasome activity is measured by fluorescence, and inhibition rates are calculated. For antiviral assays, MDCK cells are infected with Influenza A virus and treated with varying concentrations of the compound.
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| Cell Assay |
Cellular assays are performed using human MDA-MB-231 breast cancer cells treated with EGCG Octaacetate at concentrations ranging from 25 to 50 µM. Cell proliferation is assessed by MTT or SRB assay. AMPK phosphorylation is measured by Western blot. For P-glycoprotein modulation studies, MDA435/LCC6MDR cells are treated with the compound, and paclitaxel sensitivity is assessed by IC50 determination.
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| Animal Protocol |
In mouse models of colitis-driven colon cancer, EGCG Octaacetate is administered orally or intraperitoneally. Colitis is induced using DSS (dextran sulfate sodium), and colon cancer is assessed by tumor number and size. Inflammatory mediator levels are measured in colon tissue by ELISA or qPCR. PI3K/Akt/NF-κB phosphorylation and p65 acetylation are assessed by Western blot.
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| ADME/Pharmacokinetics |
EGCG Octaacetate is designed as a prodrug to enhance the stability and bioavailability of EGCG in vivo. The acetylation increases lipophilicity, improving membrane permeability and oral absorption. Once absorbed, the acetate groups are hydrolyzed to release active EGCG. The compound has high efficacy, bioavailability, and antioxidant capacities.
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| Toxicity/Toxicokinetics |
EGCG Octaacetate has demonstrated a favorable safety profile in vitro and in vivo. In cell assays, the compound shows minimal toxicity at effective concentrations. In mouse models, it is well-tolerated at doses that reduce colitis-driven colon cancer.
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| References |
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| Additional Infomation |
EGCG octaacetate is a catechin. It has been reported that EGCG octaacetate has been found in Stryphnodendron adstringens, and relevant data are available for reference.
EGCG Octaacetate is a prodrug of EGCG that enhances stability and bioavailability. It downregulates PI3K/Akt/NF-κB phosphorylation and p65 acetylation to decrease pro-inflammatory mediator levels and reduce colitis-driven colon cancer in mice. It has potential antibacterial activity against Gram-positive and Gram-negative bacteria. |
| Molecular Formula |
C38H34O19
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|---|---|
| Molecular Weight |
794.665173053741
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| Exact Mass |
794.169
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| CAS # |
148707-39-5
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| PubChem CID |
11787645
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| Appearance |
White to off-white solid powder
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| Density |
1.46±0.1 g/cm3(Predicted)
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| Boiling Point |
879.7±65.0 °C(Predicted)
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| Melting Point |
114.3-115.1 °C
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| LogP |
3.99
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
19
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| Rotatable Bond Count |
20
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| Heavy Atom Count |
57
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| Complexity |
1510
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CC(=O)OC1=CC2=C(C[C@H]([C@H](O2)C3=CC(=C(C(=C3)OC(=O)C)OC(=O)C)OC(=O)C)OC(=O)C4=CC(=C(C(=C4)OC(=O)C)OC(=O)C)OC(=O)C)C(=C1)OC(=O)C
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| InChi Key |
SVHJCTSSYQPWEV-VSJLXWSYSA-N
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| InChi Code |
InChI=1S/C38H34O19/c1-16(39)48-26-13-28(49-17(2)40)27-15-34(57-38(47)25-11-32(52-20(5)43)37(55-23(8)46)33(12-25)53-21(6)44)35(56-29(27)14-26)24-9-30(50-18(3)41)36(54-22(7)45)31(10-24)51-19(4)42/h9-14,34-35H,15H2,1-8H3/t34-,35-/m1/s1
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| Chemical Name |
[(2R,3R)-5,7-diacetyloxy-2-(3,4,5-triacetyloxyphenyl)-3,4-dihydro-2H-chromen-3-yl] 3,4,5-triacetyloxybenzoate
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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 : ~100 mg/mL (~125.84 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.15 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.2584 mL | 6.2919 mL | 12.5838 mL | |
| 5 mM | 0.2517 mL | 1.2584 mL | 2.5168 mL | |
| 10 mM | 0.1258 mL | 0.6292 mL | 1.2584 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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