| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| Other Sizes |
| Targets |
Sodium gualenate targets the stomach mucosa as a cytoprotective agent. It has anti-inflammatory and wound-healing effects. The compound has antibacterial properties. It is photomutagenic in Salmonella and causes DNA damage in human cells. Sodium gualenate has anti-allergic, anti-oxidation, and radiation protection effects.
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| ln Vitro |
At ambient temperature, the unstable chemical sodium eventually transforms into a solid state. Increasing sodium decomposes almost entirely after heating in a week. For tableting, a kneaded mixture of sodium guaiaginate and cornstarch (weight ratio: 1:250) was found to be water-stable. Consequently, during the production process, sodium guarate can be stabilized using water [1]. Sodium guarate significantly decreases leukocyte migration generated by fMLP and only weakly suppresses the production of histamine from rat peritoneal mast cells [2].
In vitro, Sodium gualenate has antibacterial properties. It causes DNA damage in human cells. The compound is a hydrophilic analogue of guaiazulene. Its anti-inflammatory and cytoprotective effects have been characterized in various in vitro systems. Sodium gualenate is used in studies of ulcer and gastritis. |
| ln Vivo |
Human gastritis is commonly treated with sodium guarinate. Sodium guarlate's primary mechanism of stomach mucosa protection is known as cytoprotection, and in vivo studies have shown its antibacterial properties [2].
In vivo, Sodium gualenate has been frequently used for the treatment of human gastritis. Its primary mechanism is cytoprotection of the stomach's mucosal lining. The compound also has antipeptic actions. It is used for the treatment of duodenal ulcer, gastric ulcer, and gastritis. It is also used clinically as a therapeutic agent for inflammation of the mouth and throat, pharyngitis, tonsillitis, stomatitis, and conjunctivitis. |
| Enzyme Assay |
In vitro enzyme assays for Sodium gualenate involve measuring its anti-inflammatory and cytoprotective effects. Anti-inflammatory activity is assessed by measuring inhibition of pro-inflammatory cytokine production. Cytoprotective effects are assessed in gastric epithelial cell models exposed to damaging agents. Antibacterial activity is assessed by MIC determination. DNA damage is assessed by comet assay. Assays are performed in appropriate buffer systems with positive controls.
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| Cell Assay |
In vitro cell-based assays for Sodium gualenate are conducted in gastric epithelial cells and other relevant cell types. Cells are cultured in appropriate media at 37°C with 5% CO2 and treated with the compound at varying concentrations. Cytoprotection is assessed by measuring cell viability after exposure to damaging agents. Inflammatory markers are measured by ELISA. Cell viability is assessed by standard assays. Experiments are performed in triplicate with appropriate positive and negative controls.
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| Animal Protocol |
Sodium gualenate in vivo studies are conducted in animal models of gastric ulcers and gastritis. Animals are treated with Sodium gualenate via oral administration. Gastric mucosal protection is assessed by measuring ulcer index and mucosal damage. For clinical applications, the compound is used in the treatment of human gastritis, duodenal ulcer, and gastric ulcer. Animals are monitored for clinical signs. Tissues are collected for histopathological analysis at study endpoints.
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| ADME/Pharmacokinetics |
Sodium gualenate (MW 300.35 g/mol, C15H17NaO3S) is a hydrophilic derivative of guaiazulene. It is also known as Guaiazulenesulfonate sodium. The compound is soluble in water and other appropriate solvents. It is stable under recommended storage conditions. Pharmacokinetic parameters such as half-life, bioavailability, and tissue distribution would be determined in species-specific studies. Sodium gualenate is used in anti-inflammatory and gastrointestinal research.
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| Toxicity/Toxicokinetics |
Sodium gualenate is generally well-tolerated at therapeutic doses. The compound is a hydrophilic derivative of guaiazulene with established safety profiles. It is photomutagenic in Salmonella and causes DNA damage in human cells. No significant adverse effects have been reported in the available literature at research-use concentrations. The compound is intended for research use only. Standard safety precautions should be followed when handling. Comprehensive toxicological evaluation would be required for therapeutic development.
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| References |
[1]. Nakamichi K, et al. Stabilization of sodium guaiazulene sulfonate in granules for tableting prepared using a twin-screw extruder. Eur J Pharm Biopharm. 2003 Nov;56(3):347-54.
[2]. Cao T, et al. Synthesis and Biological Evaluation of 3, 8-dimethyl-5-isopropylazulene Derivatives as Anti-gastric Ulcer Agent. Chem Biol Drug Des. 2016 Aug;88(2):264-71. |
| Additional Infomation |
Sodium gualenate (Guaiazulenesulfonate sodium) is a hydrophilic derivative of guaiazulene with anti-inflammatory and wound-healing effects. It is used for duodenal ulcer, gastric ulcer, and gastritis via cytoprotection of gastric mucosa. The compound also has antibacterial properties and is used for pharyngitis, tonsillitis, stomatitis, and conjunctivitis. Its molecular formula is C15H17NaO3S with a molecular weight of 300.35 g/mol. All applications are limited to non-human research use.
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| Molecular Formula |
C15H17NAO3S
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|---|---|
| Molecular Weight |
300.3485
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| Exact Mass |
300.079
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| CAS # |
6223-35-4
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| PubChem CID |
23669592
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| Appearance |
Typically exists as solid at room temperature
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| Melting Point |
98°C(lit.)
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| LogP |
4.516
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
20
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| Complexity |
415
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C1=C([H])C(C([H])([H])[H])=C2C([H])=C(C([H])=C([H])C(C([H])([H])[H])=C21)C([H])(C([H])([H])[H])C([H])([H])[H])(=O)(=O)[O-].[Na+]
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| InChi Key |
GEYJUFBPCGDENK-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C15H18O3S.Na/c1-9(2)12-6-5-10(3)15-13(8-12)11(4)7-14(15)19(16,17)18;/h5-9H,1-4H3,(H,16,17,18);/q;+1/p-1
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| Chemical Name |
sodium;3,8-dimethyl-5-propan-2-ylazulene-1-sulfonate
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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 : ~25 mg/mL (~83.24 mM)
H2O : ~6.25 mg/mL (~20.81 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.32 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 (8.32 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3294 mL | 16.6472 mL | 33.2945 mL | |
| 5 mM | 0.6659 mL | 3.3294 mL | 6.6589 mL | |
| 10 mM | 0.3329 mL | 1.6647 mL | 3.3294 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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