| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Fudosteine targets the overproduction of mucus in the airways. It inhibits MUC5AC mucin hypersecretion by reducing MUC5AC gene expression. The compound also decreases LPS-induced p-ERK1/2 and p-p38 MAPK levels in the lungs, indicating an anti-inflammatory effect. By reducing both mucus production and inflammation, fudosteine helps to alleviate respiratory symptoms in chronic bronchial disorders.
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| ln Vitro |
LPS-induced p-ERK1/2 and p-p38 MAPK levels in rat lungs are decreased by fudosteine (50, 100, and 200 mg/kg). Pretreatment with 1 mM fudosteine can prevent the rise in MUC5AC mRNA expression that is brought on by TNF-α [1].
In vitro, fudosteine (1 mM) inhibits the TNF-α-induced increase in MUC5AC mRNA expression. It decreases LPS-induced p-ERK1/2 and p-p38 MAPK levels. The compound's ability to reduce mucin gene expression and inflammatory signaling has been demonstrated in various cell-based models. These activities are central to its mechanism as a mucoactive and anti-inflammatory agent. |
| ln Vivo |
In vivo, fudosteine (50, 100, 200 mg/kg) decreases LPS-induced p-ERK1/2 and p-p38 MAPK levels in rat lungs. When given to bronchitic rabbits at an oral dose of 500 mg/kg daily, it potently decreased the fucose/N-acetylneuraminic acid in sputa, exhibiting mucoregulatory properties. The compound also suppressed blood flow of tracheal microvasculature increased by SO2 in rabbits. It prevented the development of airway hyperresponsiveness and lymphocyte accumulation in ovalbumin-challenged models.
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| Enzyme Assay |
In vitro enzyme assays for fudosteine are not typically performed, as it is a mucoactive agent rather than a direct enzyme inhibitor. Its activity is assessed by measuring its effects on mucin gene expression and inflammatory signaling pathways. The compound's ability to reduce MUC5AC mRNA levels is measured using quantitative PCR in treated cells.
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| Cell Assay |
In vitro cell-based assays for fudosteine involve treating airway epithelial cells with the compound and assessing its effects on MUC5AC gene expression. Cells are stimulated with TNF-α or other inflammatory mediators to induce mucin production. The compound's ability to reduce MUC5AC mRNA levels is measured by qPCR. Its effects on MAPK signaling pathways are assessed by Western blotting for phosphorylated ERK1/2 and p38.
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| Animal Protocol |
In vivo animal experiments for fudosteine have been conducted in rat and rabbit models of bronchitis and airway inflammation. Rats are treated with LPS to induce lung inflammation, and fudosteine is administered at doses of 50, 100, or 200 mg/kg. In bronchitic rabbits, an oral dose of 500 mg/kg daily is given. Efficacy endpoints include measurement of mucin levels in sputa, assessment of inflammatory markers, and histological analysis of airway tissues.
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| ADME/Pharmacokinetics |
Fudosteine has a molecular weight of 179.24 and a molecular formula of C6H13NO3S. It is an off-white powder with a melting point of 200-202°C (dec.). The compound is soluble in water (slightly) and is stored in a dark, inert atmosphere at -20°C. It has a pKa of 2.09±0.10. Its chemical name is (R)-2-amino-3-(3-hydroxypropylthio)propionic acid.
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| Toxicity/Toxicokinetics |
Fudosteine is a reproductive hazard. It is generally well-tolerated at therapeutic doses, as it is a clinically used mucoactive agent. Common side effects are mild and gastrointestinal in nature. Preclinical toxicology studies have been conducted to establish the safety profile for its clinical use. The compound is also known to have anti-inflammatory properties.
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| References | |
| Additional Infomation |
Fudosteine is an organic molecular entity.
Fudosteine is a cysteine derivative and a mucoactive agent launched in Japan for the treatment of bronchitis and respiratory congestion. It inhibits MUC5AC mucin hypersecretion by reducing MUC5AC gene expression. The compound also has anti-inflammatory properties. It is an anti-inflammatory expectorant used in MUC5 mucin obstructive pulmonary disease. Fudosteine is also known as S-(3-hydroxypropyl)cysteine. |
| Molecular Formula |
C6H13NO3S
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|---|---|
| Molecular Weight |
179.234
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| Exact Mass |
179.061
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| CAS # |
13189-98-5
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| PubChem CID |
134669
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
354.5±42.0 °C at 760 mmHg
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| Melting Point |
210.9-212.5ºC
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| Flash Point |
168.2±27.9 °C
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| Vapour Pressure |
0.0±1.8 mmHg at 25°C
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| Index of Refraction |
1.558
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| LogP |
-0.1
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
11
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| Complexity |
120
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C(CO)CSC[C@@H](C(=O)O)N
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| InChi Key |
KINWYTAUPKOPCQ-YFKPBYRVSA-N
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| InChi Code |
InChI=1S/C6H13NO3S/c7-5(6(9)10)4-11-3-1-2-8/h5,8H,1-4,7H2,(H,9,10)/t5-/m0/s1
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| Chemical Name |
(2R)-2-amino-3-(3-hydroxypropylsulfanyl)propanoic acid
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| Synonyms |
SS 320A; SS-320A; Fudosteine
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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) |
H2O : ≥ 100 mg/mL (~557.91 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (278.96 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 | 5.5794 mL | 27.8971 mL | 55.7942 mL | |
| 5 mM | 1.1159 mL | 5.5794 mL | 11.1588 mL | |
| 10 mM | 0.5579 mL | 2.7897 mL | 5.5794 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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