| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
Protein Tyrosine Phosphatase 1B (PTP1B) (IC50 = 6.8 μM) [2]
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|---|---|
| ln Vitro |
Silydianin exhibited antioxidant activity by scavenging reactive oxygen species (ROS) in vitro. At concentrations of 10, 25, and 50 μM, it reduced ROS levels induced by hydrogen peroxide (H₂O₂) in human skin fibroblasts by 32%, 58%, and 75% respectively, compared to the H₂O₂-only control [3]
It acted as an allosteric inhibitor of PTP1B, dose-dependently inhibiting enzyme activity with an IC50 value of 6.8 μM. The inhibition was reversible and non-competitive with the substrate, indicating binding to an allosteric site of PTP1B [2] In human keratinocytes (HaCaT cells) exposed to UVB radiation, Silydianin (5–20 μM) dose-dependently increased cell viability, reduced DNA damage (assessed by comet assay), and upregulated the expression of antioxidant enzymes (superoxide dismutase, catalase) at the protein level (detected by Western blot) [1] |
| Enzyme Assay |
For PTP1B activity assay, the reaction mixture contained recombinant PTP1B, a synthetic phosphopeptide substrate, and serial concentrations of Silydianin (1–50 μM) in a suitable buffer. The reaction was initiated by adding the substrate and incubated at 37°C for 30 minutes. The amount of free phosphate released was measured using a colorimetric method to determine enzyme activity. Kinetic analysis was performed to assess the mode of inhibition (competitive vs. non-competitive) [2]
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| Cell Assay |
Human skin fibroblasts were seeded in culture plates and incubated until 70% confluence. Cells were pre-treated with Silydianin (10, 25, 50 μM) for 2 hours, then exposed to 100 μM H₂O₂ for 1 hour to induce ROS production. Intracellular ROS levels were detected using a fluorescent ROS probe, and fluorescence intensity was measured by a microplate reader [3]
HaCaT cells were cultured to 80% confluence and pre-treated with Silydianin (5, 10, 20 μM) for 24 hours, followed by UVB irradiation (30 mJ/cm²). Cell viability was evaluated by MTT assay 24 hours post-irradiation. For DNA damage assessment, cells were processed for comet assay and visualized under a fluorescence microscope. For antioxidant enzyme detection, cells were lysed, and protein extracts were subjected to Western blot analysis [1] |
| References | |
| Additional Infomation |
Silymarin has been reported to exist in milk thistle (Silybum eburneum) and milk thistle (Silybum marianum), and there are related data reports.
Silymarin is a flavonoid lignan isolated from the seeds of milk thistle (Silybum marianum)[1][2][3] Its antioxidant mechanism involves direct scavenging of reactive oxygen species (ROS) and upregulation of the endogenous antioxidant enzyme system, which helps protect cells from damage caused by oxidative stress[1][3] As an allosteric PTP1B inhibitor, it may have potential applications in the treatment of metabolic diseases such as type 2 diabetes, because PTP1B is a key negative regulator of insulin signaling[2] It has a skin-protective effect against UVB-induced damage (including cell death and DNA damage), making it a potential candidate ingredient for skin care products or photoprotectants[1] |
| Molecular Formula |
C25H22O10
|
|---|---|
| Molecular Weight |
482.4362
|
| Exact Mass |
482.121
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| CAS # |
29782-68-1
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| PubChem CID |
11982272
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| Appearance |
White to off-white solid powder
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| Density |
1.7±0.1 g/cm3
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| Boiling Point |
819.0±65.0 °C at 760 mmHg
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| Melting Point |
191 °C
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| Flash Point |
285.0±27.8 °C
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| Vapour Pressure |
0.0±3.1 mmHg at 25°C
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| Index of Refraction |
1.747
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| LogP |
1.84
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
35
|
| Complexity |
935
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| Defined Atom Stereocenter Count |
7
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| SMILES |
COC1=C(C=CC(=C1)[C@@H]2[C@H]3CO[C@@]4([C@H]3C(=C[C@H]2C4=O)[C@@H]5[C@H](C(=O)C6=C(C=C(C=C6O5)O)O)O)O)O
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| InChi Key |
CYGIJEJDYJOUAN-JSGXPVSSSA-N
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| InChi Code |
InChI=1S/C25H22O10/c1-33-16-4-9(2-3-14(16)27)18-11-7-12(20-13(18)8-34-25(20,32)24(11)31)23-22(30)21(29)19-15(28)5-10(26)6-17(19)35-23/h2-7,11,13,18,20,22-23,26-28,30,32H,8H2,1H3/t11-,13-,18+,20+,22+,23-,25-/m1/s1
|
| Chemical Name |
(1R,3R,6R,7R,10R)-3-hydroxy-10-(4-hydroxy-3-methoxyphenyl)-8-[(2R,3R)-3,5,7-trihydroxy-4-oxo-2,3-dihydrochromen-2-yl]-4-oxatricyclo[4.3.1.03,7]dec-8-en-2-one
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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 : ~125 mg/mL (~259.10 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.31 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 20.8 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: ≥ 2.08 mg/mL (4.31 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 20.8 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: ≥ 2.08 mg/mL (4.31 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 | 2.0728 mL | 10.3640 mL | 20.7280 mL | |
| 5 mM | 0.4146 mL | 2.0728 mL | 4.1456 mL | |
| 10 mM | 0.2073 mL | 1.0364 mL | 2.0728 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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