| Size | Price | Stock | Qty |
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| 50mg |
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| Other Sizes |
| Targets |
Norathyriol targets multiple enzymes and receptors. It is a potent, noncompetitive inhibitor of α-glucosidase, an enzyme that breaks down carbohydrates into glucose, making it a potential agent for managing postprandial blood sugar levels. It also inhibits the peroxisome proliferator-activated receptors PPARα, PPARβ, and PPARγ with IC50 values of 92.8 µM, suggesting a role in lipid metabolism and insulin sensitivity. Additionally, it exhibits inhibitory activity against protein kinase C.
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| ln Vitro |
Norathyrol (1-25 µM) stops JB6 P+ cells from growing by causing a cell cycle arrest. Norathyrol causes G2-M arrest, which stops JB6 cell development [3]. In JB6 P+ cells, northyronol prevents UVB-induced ERK phosphorylation, AP-1, and NF-κB activation [3] [WB cell growth assay].
In vitro, norathyriol demonstrates potent inhibition of α-glucosidase with an IC50 of 3.12 μM. This noncompetitive inhibition suggests it binds to a site on the enzyme distinct from the active site. It also inhibits PPARα, PPARβ, and PPARγ with IC50s of 92.8 µM. These activities make it a useful tool for studying carbohydrate metabolism and insulin signaling. |
| ln Vivo |
Northiol is a natural metabolite of mango in the human gut and is oral effective and safe [1]. Northyronol (0.92, 1.85 and 3.7 mg/kg) dose-dependently lowered serum uric acid levels by 27.0%, 33.6 and 37.4%, respectively [4].
In vivo, norathyriol is noted for its good cell permeability and oral availability, suggesting it can be effectively absorbed and distributed. These properties make it a promising candidate for in vivo studies of diabetes and metabolic disorders. Specific animal studies, including dosing and administration routes, are not detailed in the provided literature but are likely reported in other sources on this compound. |
| Enzyme Assay |
The inhibitory activity of norathyriol is typically assessed using cell-free enzymatic assays. For α-glucosidase, the enzyme is incubated with a substrate (e.g., p-nitrophenyl-α-D-glucopyranoside) and varying concentrations of the inhibitor. The production of the chromophore p-nitrophenol is measured spectrophotometrically, and the IC50 is calculated. Its noncompetitive mechanism is confirmed by varying the substrate concentration. PPAR activity can be assessed using reporter gene assays or binding assays.
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| Cell Assay |
cell viability assay [3]
Cell Types: Mouse skin epidermis JB6 P+ cells Tested Concentrations: 0 , 1, 10 or 25 µM Incubation Duration: 24 or 72 hrs (hours) Experimental Results: Inhibits cell growth in a dose- and time-dependent manner without causing cell death. Western Blot Analysis[3] Cell Types: JB6 P+ Cell Tested Concentrations: 0, 1, 10 or 25 µM Incubation Duration: 2 hrs (hours) Experimental Results: Inhibition of UVB-induced ERK and p90RSK phosphorylation. The cellular activity of norathyriol can be evaluated in various cell lines, such as those involved in glucose or lipid metabolism. Its effect on glucose uptake, glycogen synthesis, or adipocyte differentiation can be measured. Its ability to activate PPARs can be confirmed using reporter gene assays in cell lines expressing these receptors. |
| Animal Protocol |
Animal/Disease Models: Adult Kunming mice, body weight 18-22 g[4]
Doses: 0.92, 1.85 and 3.7 mg/kg Route of Administration: intragastric (po) (po)administration; twice a day for a total of five times. Experimental Results: Serum uric acid levels diminished by 27.0% respectively. , 33.6% and 37.4%. In animal studies, norathyriol would typically be administered orally or intraperitoneally to rodent models of diabetes or metabolic syndrome. Its effect on blood glucose levels, insulin sensitivity, and lipid profiles would be measured. Pharmacodynamic markers, such as the activity of α-glucosidase in the intestine, could also be assessed. |
| ADME/Pharmacokinetics |
Norathyriol is noted for its good oral availability and cell permeability, which are key features for its potential as a therapeutic agent. However, detailed pharmacokinetic parameters, such as half-life and volume of distribution, are not provided in the available literature. Its solubility in DMSO (90 mg/mL) is reported, which facilitates its use in in vitro experiments.
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| Toxicity/Toxicokinetics |
Toxicology data for norathyriol is not provided in the available literature. However, as a natural metabolite with good oral availability, it is presumed to have a favorable safety profile. The compound is for research use only and not for human therapeutic applications without further study.
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| References |
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| Additional Infomation |
Norathyriol is an oxacyclohexanone compound with the structure 9H-oxacyclohexanone-9-one, substituted with hydroxyl groups at positions 1, 3, 6, and 7. It was isolated from Garcinia mangostana and Maclura pomifera and possesses inhibitory activity against protein kinase C. Norathyriol is used as an antitumor drug, an EC 2.7.11.13 (protein kinase C) inhibitor, and a plant metabolite. It belongs to the oxacyclohexanone class and the polyphenol class. Norathyriol has been reported to exist in Garcinia cowa, Hypericum sampsonii, and other organisms with relevant data.
Norathyriol (Mangiferitin, CAS: 3542-72-1) is a naturally occurring xanthone with promising bioactivity. Its potent, noncompetitive inhibition of α-glucosidase and its ability to inhibit PPARs make it a valuable research tool for studying diabetes and metabolic syndrome. Its good oral availability and cell permeability further enhance its utility as a lead compound for drug discovery. |
| Molecular Formula |
C13H8O6
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|---|---|
| Molecular Weight |
260.20
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| Exact Mass |
260.032
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| CAS # |
3542-72-1
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| PubChem CID |
5281656
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| Appearance |
White to off-white solid powder
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| Density |
1.8±0.1 g/cm3
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| Boiling Point |
595.1±50.0 °C at 760 mmHg
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| Flash Point |
237.8±23.6 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.801
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| LogP |
0.95
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
19
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| Complexity |
372
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ZHTQCPCDXKMMLU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H8O6/c14-5-1-9(17)12-11(2-5)19-10-4-8(16)7(15)3-6(10)13(12)18/h1-4,14-17H
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| Chemical Name |
1,3,6,7-tetrahydroxyxanthen-9-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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 (~384.32 mM)
H2O: < 0.1 mg/mL (Insoluble) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.61 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 (9.61 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 (9.61 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 | 3.8432 mL | 19.2160 mL | 38.4320 mL | |
| 5 mM | 0.7686 mL | 3.8432 mL | 7.6864 mL | |
| 10 mM | 0.3843 mL | 1.9216 mL | 3.8432 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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