| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
- 5-Hydroxytryptamine 2A (5-HT₂A) receptor (Ki = 0.3 μM)[1]
- Amyloid-beta (Aβ) aggregation and production-related targets [2] |
|---|---|
| ln Vitro |
- Rat aortic strips: Gamma-Mangostin acts as a selective 5-HT₂A receptor antagonist, dose-dependently inhibiting 5-HT-induced vasoconstriction with maximal inhibition rate of ~80% at 1 μM[1]
- SH-SY5Y cells: Gamma-Mangostin inhibits Aβ₁₋₄₂ aggregation with an IC₅₀ of 12.5 μM, and reduces Aβ₁₋₄₀/Aβ₁₋₄₂ production by suppressing cleavage of amyloid precursor protein (APP) via downregulating BACE1 expression[2] - 3T3-L1 adipocytes (insulin-resistant model): Gamma-Mangostin (10, 20 μM) enhances insulin sensitivity, promoting glucose uptake by 30-45% compared to control, and upregulates GLUT4 membrane translocation[5] |
| ln Vivo |
- STZ-induced diabetic mice: Oral administration of Gamma-Mangostin (20, 40 mg/kg/day for 4 weeks) improves liver function, reducing serum ALT and AST levels by 40-60%, and alleviates hepatic steatosis and inflammatory infiltration[3]
- STZ-induced diabetic mice: Gamma-Mangostin (20, 40 mg/kg/day, oral for 4 weeks) exerts renal protective effects, decreasing serum creatinine and urea nitrogen levels by 35-55%, and attenuating renal glomerular hypertrophy, tubular damage, and interstitial fibrosis[4] - STZ-induced diabetic mice: Gamma-Mangostin (20, 40 mg/kg/day, oral for 4 weeks) synergizes with insulin to lower fasting blood glucose (by 30-50%) and glycated hemoglobin (HbA₁c) levels, and enhances insulin signaling via increasing Akt phosphorylation in liver and muscle tissues[5] |
| Enzyme Assay |
- 5-HT₂A receptor competitive binding assay: Membrane preparations from rat brain cortex expressing 5-HT₂A receptor are incubated with radiolabeled 5-HT and various concentrations of Gamma-Mangostin (0.01-10 μM) at 25°C for 60 minutes. Bound radioligand is separated by filtration, and radioactivity is measured. Ki value is calculated via nonlinear regression analysis of competition binding curves[1]
- Aβ aggregation inhibition assay: Aβ₁₋₄₂ peptide is incubated with Gamma-Mangostin (5-50 μM) at 37°C for 48 hours. Thioflavin T (ThT) fluorescent probe is added, and fluorescence intensity is detected at excitation wavelength 440 nm and emission wavelength 485 nm to evaluate Aβ aggregation degree, with IC₅₀ value calculated[2] |
| Cell Assay |
- Rat aortic strip contraction assay: Isolated rat thoracic aortic strips are suspended in Krebs-Ringer bicarbonate buffer (37°C, aerated with 95% O₂ and 5% CO₂) and equilibrated for 60 minutes. Vasoconstriction is induced by 5-HT (1 μM), followed by addition of Gamma-Mangostin (0.1-1 μM). Contractile tension is recorded via a force transducer, and inhibition rate is calculated[1]
- Aβ production detection assay: SH-SY5Y cells are seeded in 6-well plates and cultured to 70% confluence. Cells are treated with Gamma-Mangostin (5-20 μM) for 24 hours. Cell supernatants and lysates are collected; Aβ₁₋₄₀/Aβ₁₋₄₂ concentrations are measured by ELISA, and APP/BACE1 protein expressions are detected by Western blot[2] - Glucose uptake assay: Differentiated 3T3-L1 adipocytes are induced to insulin resistance. Cells are treated with Gamma-Mangostin (10, 20 μM) and insulin (10 nM) for 12 hours. Fluorescently labeled 2-deoxyglucose is added, and intracellular fluorescence intensity is measured to quantify glucose uptake[5] |
| Animal Protocol |
- Diabetic mice hepatoprotective study: Male mice are intraperitoneally injected with streptozotocin (STZ) to establish diabetic models. Mice are randomly divided into control group, Gamma-Mangostin low-dose group (20 mg/kg) and high-dose group (40 mg/kg). The test compound is administered orally once daily for 4 weeks. Serum ALT and AST levels are detected; liver tissues are collected for HE staining and immunohistochemical detection of inflammatory factors[3]
- Diabetic mice nephroprotective study: STZ-induced diabetic mice are grouped and administered Gamma-Mangostin as described in the hepatoprotective study for 4 weeks. Serum creatinine and urea nitrogen levels are measured; kidney tissues are subjected to PAS staining and Masson staining to evaluate tissue damage and fibrosis[4] - Diabetic mice hypoglycemic study: STZ-induced diabetic mice are randomly divided into control group, insulin group, and insulin + Gamma-Mangostin groups (20, 40 mg/kg). Insulin is injected subcutaneously, and Gamma-Mangostin is administered orally once daily for 4 weeks. Fasting blood glucose is measured weekly; HbA₁c and insulin levels are detected at the end of the study, and Akt phosphorylation in liver and muscle tissues is analyzed[5] |
| Toxicity/Toxicokinetics |
In vivo toxicity: Oral administration of γ-dextrin (20, 40 mg/kg/day for 4 weeks) did not cause significant systemic toxicity in diabetic mice, which showed stable weight, no significant histological damage to the heart, spleen and other major organs, and normal serum biochemical indicators [3][4][5].
|
| References | |
| Additional Infomation |
γ-Oxanthoside belongs to the xanthonesone class of compounds with the structure 9H-xanthonesone, substituted with hydroxyl groups at positions 1, 3, 6 and 7, substituted with a carbonyl group at position 9, and substituted with isopentenyl groups at positions 2 and 8. This compound was isolated from the stem of hawthorn (Cratoxylum cochinchinense) and has antitumor activity. It can function as an antitumor drug, a protein kinase inhibitor and a plant metabolite. It belongs to the xanthonesone class and phenolic class of compounds.
γ-Oxanthoside has been reported to exist in xipshuanbannaensis, Hypericum perforatum and other organisms with relevant data. See also: mangosteen pericarp (partial). -γ-Oxanthoside is a natural flavonoid compound isolated from the pericarp of mangosteen (Garcinia mangostana)[3][5]. - Its mechanisms of action include selective antagonism of 5-HT₂A receptors[1], inhibition of Aβ aggregation and APP cleavage[2], activation of insulin signaling pathways to enhance insulin sensitivity[5], and reduction of diabetes-related liver and kidney damage through anti-inflammatory and antioxidant effects[3][4]. - It has potential therapeutic value for 5-HT₂A receptor-related diseases, Alzheimer's disease, and complications of diabetes. (Liver and kidney diseases)[1][2][3][4][5] |
| Molecular Formula |
C23H24O6
|
|---|---|
| Molecular Weight |
396.4331
|
| Exact Mass |
396.157
|
| CAS # |
31271-07-5
|
| PubChem CID |
5464078
|
| Appearance |
Light yellow to yellow solid powder
|
| Density |
1.3±0.1 g/cm3
|
| Boiling Point |
648.4±55.0 °C at 760 mmHg
|
| Melting Point |
207 °C
|
| Flash Point |
226.4±25.0 °C
|
| Vapour Pressure |
0.0±2.0 mmHg at 25°C
|
| Index of Refraction |
1.656
|
| LogP |
5.14
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
29
|
| Complexity |
662
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
VEZXFTKZUMARDU-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C23H24O6/c1-11(2)5-7-13-15(24)9-18-20(22(13)27)23(28)19-14(8-6-12(3)4)21(26)16(25)10-17(19)29-18/h5-6,9-10,24-27H,7-8H2,1-4H3
|
| Chemical Name |
1,3,6,7-tetrahydroxy-2,8-bis(3-methylbut-2-enyl)xanthen-9-one
|
| 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 (~252.25 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.31 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 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 (6.31 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 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 (6.31 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 | 2.5225 mL | 12.6126 mL | 25.2251 mL | |
| 5 mM | 0.5045 mL | 2.5225 mL | 5.0450 mL | |
| 10 mM | 0.2523 mL | 1.2613 mL | 2.5225 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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