| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
| Targets |
Taxifolin has multiple targets. It binds at the ATP-binding site on VEGFR-2 kinase and acts as a type I competitive inhibitor. It exhibits anti-tyrosinase activity. It significantly inhibits collagenase with an IC50 value of 193.3 µM. It inhibits fatty acid synthesis and cell growth and induces apoptosis.
|
|---|---|
| ln Vitro |
Studies on collagenase activity using (+)-catechin and pure paclitaxel supported this. (+)-catechin was inert, however taxifolin exhibited strong inhibitory effect with an IC50 value of 193.3 μM [1]. A common bioactive component of foods and natural remedies is taxifol. A bioactive flavanol called taxifolin (dihydroquercetin) is frequently present in milk thistle, French marine bark, Douglas fir bark, onions, grapes, citrus fruits, green tea, olive oil, wine, and many other foods [3].
In vitro, taxifolin exhibits significant inhibitory activity against collagenase with an IC50 value of 193.3 µM. It exhibits important anti-tyrosinase activity. It binds at the ATP-binding site on VEGFR-2 kinase as a type I competitive inhibitor. It inhibits fatty acid synthesis and cell growth and induces apoptosis. |
| ln Vivo |
Taxifol is believed to be easily metabolized, and its metabolites are the forms that are widely found in the body, despite the paucity of evidence on its in vivo metabolism [3].
In vivo, taxifolin displays cardioprotective, neuroprotective, and anticancer chemotherapeutic activities. It inhibits proliferation of cancer cells in vitro and in vivo. It has antioxidant effects and may protect against oxidative damage. It has been studied for its antifibrotic effects. |
| Enzyme Assay |
In vitro enzyme assays for taxifolin measure its inhibition of collagenase (IC50=193.3 µM) and tyrosinase. VEGFR-2 kinase inhibition is assessed using ATP-competitive binding assays. Antioxidant activity is measured using DPPH radical scavenging or other standard assays. The compound's ability to inhibit fatty acid synthesis is measured in cell-free systems.
|
| Cell Assay |
In vitro cell-based assays for taxifolin use various cancer cell lines to assess anti-proliferative and pro-apoptotic effects. Cells are treated with serial dilutions of the compound, and cell viability is measured using MTT or other assays. Apoptosis is assessed by annexin V staining or caspase activity assays. Fatty acid synthesis inhibition is measured by incorporation of labeled precursors.
|
| Animal Protocol |
In vivo animal models for taxifolin include models of cancer, cardiovascular disease, and neurological disorders. The compound is administered orally or intraperitoneally, and its effects on tumor growth, cardiac function, and neuroprotection are evaluated. Antifibrotic effects are assessed in models of fibrosis.
|
| ADME/Pharmacokinetics |
Taxifolin has a molecular formula of C₁₅H₁₂O₇ and a molecular weight of 304.25 g/mol. It is also known as (+)-Dihydroquercetin, Taxifoliol, and (+)-Taxifolin. It is a catechol-type flavonoid. The compound is soluble in DMSO and ethanol. It is stored under appropriate conditions for research use.
|
| Toxicity/Toxicokinetics |
Taxifolin is a natural compound with a favorable safety profile. It is generally well-tolerated at therapeutic doses. The compound is for research use only and is not approved for clinical use. Appropriate safety precautions should be taken during handling.
|
| References |
|
| Additional Infomation |
(+)-Taxolin is a taxolin with a (2R,3R) configuration. It is a metabolite, the conjugate acid of (+)-taxolin (1-), and the enantiomer of (-)-taxolin. Taxolin has been reported in camellia (Camellia reticulata), Japanese birch (Betula platyphylla var. japonica), and other organisms with relevant data. See also: milk thistle (partial); sea pine (partial).
Taxifolin ((+)-Dihydroquercetin) is a catechol-type flavonoid with cardioprotective, neuroprotective, antioxidative, and anticancer activities. It inhibits collagenase (IC50=193.3 µM) and binds to VEGFR-2 kinase as a type I competitive inhibitor. It inhibits fatty acid synthesis and cell growth and induces apoptosis. Taxifolin is also known as (+)-Dihydroquercetin. |
| Molecular Formula |
C15H12O7
|
|---|---|
| Molecular Weight |
304.25
|
| Exact Mass |
304.058
|
| CAS # |
480-18-2
|
| Related CAS # |
(±)-Taxifolin;24198-97-8;(-)-Taxifolin;111003-33-9;Taxifolin-d3
|
| PubChem CID |
439533
|
| Appearance |
Off-white to yellow solid powder
|
| Density |
1.7±0.1 g/cm3
|
| Boiling Point |
687.6±55.0 °C at 760 mmHg
|
| Melting Point |
230-233°C (dec.)
|
| Flash Point |
264.2±25.0 °C
|
| Vapour Pressure |
0.0±2.3 mmHg at 25°C
|
| Index of Refraction |
1.763
|
| LogP |
1.82
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
22
|
| Complexity |
428
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
C1=CC(=C(C=C1[C@@H]2[C@H](C(=O)C3=C(C=C(C=C3O2)O)O)O)O)O
|
| InChi Key |
CXQWRCVTCMQVQX-LSDHHAIUSA-N
|
| InChi Code |
InChI=1S/C15H12O7/c16-7-4-10(19)12-11(5-7)22-15(14(21)13(12)20)6-1-2-8(17)9(18)3-6/h1-5,14-19,21H/t14-,15+/m0/s1
|
| Chemical Name |
(2R,3R)-2-(3,4-dihydroxyphenyl)-3,5,7-trihydroxy-2,3-dihydrochromen-4-one
|
| Synonyms |
Lariksin; Taxifoliol; Taxifolin
|
| 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 |
| 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 : ≥ 100 mg/mL (~328.68 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (9.04 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 27.5 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: ≥ 2.75 mg/mL (9.04 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 27.5 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: ≥ 2.75 mg/mL (9.04 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 | 3.2868 mL | 16.4339 mL | 32.8677 mL | |
| 5 mM | 0.6574 mL | 3.2868 mL | 6.5735 mL | |
| 10 mM | 0.3287 mL | 1.6434 mL | 3.2868 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.
Link: https://clinicaltrials.gov/ct2/show/NCT05190432
Conditions:Antioxidative Stress|Cold|Influenza|Aging|Inflammation