| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| 10g |
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| Other Sizes |
| Targets |
As a mucolytic expectorant, potassium guaiacolsulfonate does not have a specific molecular target in the classical sense of enzyme or receptor inhibition. Its primary action is physicochemical, working directly on respiratory mucus to reduce its viscosity and surface tension. This facilitates the clearance of mucus from the airways by ciliary action and coughing. The compound acts locally in the respiratory tract after oral administration and systemic absorption, rather than binding to a specific protein target. Its mechanism is based on increasing the water content of mucus, thereby thinning secretions and promoting expectoration.
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| ln Vitro |
In order to make coughing up mucus (phlegm) less sticky and easier, potassium guaiacolsulfonate hemihydrate thins it out in the lungs[1].
In vitro studies demonstrate that potassium guaiacolsulfonate exhibits mucolytic activity by reducing the viscosity of mucus samples in controlled laboratory settings. The compound’s ability to thin mucus has been characterized using standard viscometry assays, where it shows a concentration-dependent reduction in mucus elasticity and viscosity. It is also evaluated for its stability and solubility in various pharmaceutical formulations. The in vitro activity is typically measured by assessing the decrease in sputum viscosity or by observing the dispersal of mucus in aqueous solutions, confirming its role as an effective expectorant agent. |
| ln Vivo |
In vivo, potassium guaiacolsulfonate hemihydrate is administered orally and exerts its expectorant effects systemically after absorption. Animal model studies have demonstrated its efficacy in increasing respiratory tract fluid output and facilitating mucus clearance. The compound is used in combination with other active ingredients to treat cough associated with common cold, infections, or allergies. Its in vivo activity is primarily observed as a reduction in cough frequency and severity, and improvement in breathing parameters in models of respiratory distress. Clinical use confirms its effectiveness as a symptomatic expectorant.
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| Enzyme Assay |
For in vitro enzyme/receptor binding studies unrelated to cell-based assays, potassium guaiacolsulfonate is generally not evaluated against specific enzymes or receptors due to its non-targeted mucolytic mechanism. Standard physicochemical assays are employed to characterize its activity, including measurement of surface tension reduction and viscosity changes in simulated mucus or sputum samples. These assays typically involve mixing the compound with artificial or biological mucus preparations and assessing rheological properties using viscometers or rheometers at controlled temperatures, with results compared to untreated controls to establish concentration-response relationships.
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| Cell Assay |
In vitro cellular assays for potassium guaiacolsulfonate are not typically performed since its mechanism does not involve cellular receptors or signaling pathways. Instead, its activity is evaluated using non-cellular systems such as mucus simulants or isolated sputum samples. When cellular assays are conducted, they generally focus on toxicity or irritation potential rather than efficacy. For respiratory cell lines (e.g., bronchial epithelial cells), the compound is tested at various concentrations to assess cell viability (MTT assay) and any potential pro-inflammatory or anti-inflammatory effects, though such studies are not standard for this established expectorant.
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| Animal Protocol |
In vivo animal studies for potassium guaiacolsulfonate involve oral administration in rodent models to evaluate its expectorant efficacy. Typically, animals are dosed with the compound, and respiratory secretions are collected and measured for volume and viscosity changes. Standard protocols use phenol red secretion as a marker for airway fluid production, where the compound is administered orally, followed by intraperitoneal phenol red injection, and the dye content in tracheal washes is quantified spectrophotometrically. These studies help confirm the compound’s ability to increase respiratory tract fluid output and facilitate mucus clearance.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of potassium guaiacolsulfonate hemihydrate indicate that it is well absorbed from the gastrointestinal tract after oral administration. It is metabolized in the liver and excreted primarily via the kidneys in urine. The compound reaches peak plasma concentrations within a few hours post-administration. Its half-life is relatively short, supporting its use in multiple daily dosing regimens for symptomatic relief. The hemihydrate form enhances its stability and solubility in aqueous formulations, making it suitable for oral syrups and solutions commonly used in respiratory care.
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| Toxicity/Toxicokinetics |
Toxicological data for potassium guaiacolsulfonate hemihydrate indicate that it is well-tolerated at therapeutic doses with a low incidence of adverse effects. Common side effects may include mild gastrointestinal upset or allergic reactions in sensitive individuals. In chronic toxicity studies, the compound does not show significant organ toxicity or carcinogenic potential at clinically relevant doses. It is classified as safe for use in over-the-counter expectorant products, with a wide therapeutic index. Overdose may lead to nausea, vomiting, or diarrhea, but serious toxicity is rare. Standard safety assessments confirm its acceptable profile for human use.
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| References |
[1]. Thi Huong Hoa Le, et al. Development and Validation of an HPLC Method for Simultaneous Assay of Potassium Guaiacolsulfonate and Sodium Benzoate in Pediatric Oral Powder. J Anal Methods Chem. 2019 Mar 7;2019:6143061.
[2]. Ozlem Aksu Dönmez, et al. Simultaneous Determination of Potassium Guaiacolsulfonate, Guaifenesin, Diphenhydramine HCl and Carbetapentane Citrate in Syrups by Using HPLC-DAD Coupled With Partial Least Squares Multivariate Calibration. Talanta. 2011 Feb 15;83(5):1601-5. |
| Additional Infomation |
Potassium guaiacolsulfonate hemihydrate is a widely used expectorant available in many over-the-counter cough and cold preparations, often combined with decongestants, antihistamines, or antitussives. It is regulated as a pharmaceutical ingredient in multiple jurisdictions and has a long history of safe use in symptomatic respiratory care. The compound is stable under normal storage conditions and is formulated in syrups, solutions, and pediatric preparations. It is not considered a curative treatment but rather a supportive therapy for managing productive cough associated with various respiratory conditions. Its mechanism is physicochemical rather than receptor-mediated.
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| Molecular Formula |
C7H8O5S.1/2H2O.K
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| Molecular Weight |
251.31
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| Exact Mass |
501.94
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| CAS # |
78247-49-1
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| Related CAS # |
guaiacolsulfonate;7134-11-4
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| PubChem CID |
102601439
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
2.707
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
15
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| Complexity |
260
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1(S([O-])(=O)=O)=CC=C(O)C(OC)=C1.[K+].C1(S([O-])(=O)=O)=CC=C(O)C(OC)=C1.[K+].O
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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) |
H2O : 62.5 mg/mL (248.70 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (397.91 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9791 mL | 19.8957 mL | 39.7915 mL | |
| 5 mM | 0.7958 mL | 3.9791 mL | 7.9583 mL | |
| 10 mM | 0.3979 mL | 1.9896 mL | 3.9791 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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