| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| Other Sizes |
| Targets |
(-)-Epiafzelechin is a COX inhibitor with antioxidant and anti-inflammatory activity. It has osteoprotective effects in a mature ovariectomized mouse model, with the ability to stimulate osteoblast activity and inhibit osteoclast activity. It exhibits various modes of action in suppressing HSV-2 multiplication.
|
|---|---|
| ln Vitro |
In vitro, (-)-Epiafzelechin shows potent antioxidant activity with an EC50 of 20.9 μM (EC50=5.7 μg/mL). It is a COX inhibitor. It stimulates osteoblast activity and inhibits osteoclast activity. It suppresses HSV-2 multiplication.
|
| ln Vivo |
In vivo, (-)-Epiafzelechin protects against ovariectomy-induced bone loss in adult mice. It has osteoprotective effects. Its COX inhibitory and antioxidant activities suggest potential anti-inflammatory effects. It can be used to study rheumatoid arthritis.
|
| Enzyme Assay |
Cell-free assays for (-)-Epiafzelechin: COX-1 and COX-2 inhibition are measured using COX inhibitor screening assay kits. The enzyme is incubated with arachidonic acid and varying concentrations of the compound (0.1-100 µM). Prostaglandin production is measured by ELISA or colorimetric methods. IC50 values are calculated. Antioxidant activity is measured using DPPH, ABTS, and FRAP assays.
|
| Cell Assay |
Cellular assays for (-)-Epiafzelechin: osteoblasts and osteoclasts are cultured and treated with (-)-Epiafzelechin at concentrations of 0.1-100 µM for 24-72 hours. Osteoblast activity is assessed by measuring alkaline phosphatase activity and mineralization. Osteoclast activity is assessed by measuring TRAP activity and bone resorption pit formation. Cell viability is measured by MTT assay. Antiviral activity is assessed in HSV-2-infected cell cultures.
|
| Animal Protocol |
In vivo animal studies for (-)-Epiafzelechin: ovariectomized mouse models are used to evaluate osteoprotective effects. Animals are administered (-)-Epiafzelechin orally at doses of 10-50 mg/kg for 4-8 weeks. Bone mineral density is measured by DEXA. Bone histomorphometry and serum bone turnover markers are assessed. Anti-inflammatory effects are evaluated in models of rheumatoid arthritis.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of (-)-Epiafzelechin: as a small flavonoid (MW 274.27), it may have moderate oral bioavailability. It is likely metabolized in the liver and excreted via the kidneys. Soluble in DMSO. Storage: powder at -20°C for up to 3 years. Purity: >95%.
|
| Toxicity/Toxicokinetics |
Toxicity of (-)-Epiafzelechin: comprehensive toxicity data are limited. As a natural flavonoid, it is generally considered safe at moderate doses. It is for research use only and not approved for clinical use.
|
| References |
|
| Additional Infomation |
(-)-Epicatechin is a catechin derivative with a (2R,3R) configuration and is a plant metabolite. It has been reported to be found in tea plants, Celastrus orbiculatus, and other organisms with relevant data.
(-)-Epiafzelechin is a research compound with potential applications in bone health, inflammation, and antiviral research. It is a COX inhibitor and antioxidant. Its mechanism involves COX inhibition, antioxidant activity, and modulation of bone cell function. No clinical trials or FDA approvals have been reported. |
| Molecular Formula |
C15H14O5
|
|---|---|
| Molecular Weight |
274.27
|
| Exact Mass |
274.084
|
| CAS # |
24808-04-6
|
| PubChem CID |
443639
|
| Appearance |
White to off-white solid
|
| Density |
1.5±0.1 g/cm3
|
| Boiling Point |
583.4±50.0 °C at 760 mmHg
|
| Melting Point |
240 - 243 °C
|
| Flash Point |
306.6±30.1 °C
|
| Vapour Pressure |
0.0±1.7 mmHg at 25°C
|
| Index of Refraction |
1.709
|
| LogP |
1.09
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
20
|
| Complexity |
328
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
OC1C=CC([C@H]2OC3=CC(=CC(O)=C3C[C@H]2O)O)=CC=1
|
| InChi Key |
RSYUFYQTACJFML-UKRRQHHQSA-N
|
| InChi Code |
InChI=1S/C15H14O5/c16-9-3-1-8(2-4-9)15-13(19)7-11-12(18)5-10(17)6-14(11)20-15/h1-6,13,15-19H,7H2/t13-,15-/m1/s1
|
| Chemical Name |
(2R,3R)-2-(4-hydroxyphenyl)-3,4-dihydro-2H-chromene-3,5,7-triol
|
| Synonyms |
(-)-Epiafzelechin
|
| 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: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 (182.30 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.12 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 (9.12 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 (9.12 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 | 3.6460 mL | 18.2302 mL | 36.4604 mL | |
| 5 mM | 0.7292 mL | 3.6460 mL | 7.2921 mL | |
| 10 mM | 0.3646 mL | 1.8230 mL | 3.6460 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.