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| 5mg |
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| 50mg |
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| Targets |
Stepronin is an orally active expectorant and mucolytic agent. It primarily targets airway epithelial cells to facilitate mucus clearance. The compound exerts its biological activity by inhibiting chloride secretion from epithelial cells, leading to a reduction in mucus glycoprotein secretion from submucosal glands. This reduces airway secretion and helps to thin thick bronchial secretions. Stepronin's mechanism of action involves the modulation of ion transport and mucus production in the airways.
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| ln Vitro |
In canine tracheal epithelium, stepronin (0.1-100 µM; 20 minutes) dramatically lowers ISOP (isoproterenol)-induced SCC (short circuit current) values in a dose-dependent manner [1]. In canine tracheal epithelium, stepronin (10-100 µM; 20 minutes) substantially and dose-dependently suppresses basal secretion and ISOP-induced PD (potential difference) values [1]. Stepronin (100 µM; 20 min) dramatically reduces the amount of [3H]-glycoconjugates that submucosal glands secrete in response to ISOP [1].
In vitro, Stepronin inhibits airway secretion by reducing Cl- secretion from epithelial cells and mucus glycoprotein secretion from submucosal glands. In canine tracheal epithelium, Stepronin (0.1-100 µM) dose-dependently reduces isoproterenol-stimulated short-circuit current values, basal secretion, and isoproterenol-induced potential differences. Its in vitro activity is characterized by potent inhibition of airway secretion and mucus production. Stepronin's effects on epithelial cells and submucosal glands contribute to its expectorant activity. |
| ln Vivo |
In vivo, Stepronin is an orally active expectorant, although inhalation administration is preferable. It is used as a mucolytic and expectorant agent to facilitate mucus clearance in respiratory conditions. Expectorants increase bronchial secretions and help to thin thick bronchial secretions. Stepronin's in vivo efficacy is attributed to its ability to reduce airway secretion and mucus production. The compound's oral and inhalation routes of administration provide flexibility in its use.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays are not typically performed for Stepronin, as it acts by modulating ion transport and mucus secretion rather than binding to specific enzymes or receptors. However, its effects on chloride secretion can be studied using Ussing chamber techniques with epithelial tissues. These assays measure the compound's ability to modulate ion transport and short-circuit current in airway epithelial cells.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: Canine tracheal epithelium (from adult dogs and male-female mongrel dogs weighing 10 to 25 kg) Tested Concentrations: 0.1-100 µM; 10-100 µM Incubation Duration: 20 minutes (pretreatment) Experimental Results: Significant Dramatically inhibited ISOP-induced SCC and PD values as well as basal secretion. Cell viability assay[1] Cell Types: Submucosal gland (from adult and male-female mongrel dogs weighing 10 to 25 kg) Tested Concentrations: 100 µM Incubation Duration: 20 minutes (pre-treatment) Experimental Results: Significant inhibition of ISOP-induced [3H ]-glycoconjugate secretion. In vitro cellular assays for Stepronin typically involve treating airway epithelial cells with the compound and measuring chloride secretion and mucus glycoprotein production. In canine tracheal epithelium, Stepronin (0.1-100 µM) dose-dependently reduces isoproterenol-stimulated short-circuit current values and basal secretion. These cell-based studies demonstrate the compound's ability to inhibit airway secretion and mucus production. Stepronin's effects on epithelial cells and submucosal glands contribute to its expectorant activity. |
| Animal Protocol |
In vivo animal models for Stepronin may include models of airway hypersecretion or mucus production, such as those induced by irritants or infection. The compound is administered orally or by inhalation, and airway secretion and mucus production are measured. Stepronin's ability to reduce airway secretion and facilitate mucus clearance is assessed. However, detailed animal protocol information for Stepronin is limited in the available literature. The compound is primarily used as a research tool for studying airway secretion and expectorant activity.
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| ADME/Pharmacokinetics |
Stepronin is a synthetic N-acyl-alpha amino acid with the IUPAC name N-(1-oxo-2-((2-thienylcarbonyl)thio)propyl)glycine. The compound is typically stored under appropriate conditions to maintain stability. Its physicochemical properties support its use in both in vitro and in vivo studies. Stepronin's solubility and formulation for administration should be optimized based on specific experimental requirements. The compound is an expectorant and is used for research purposes.
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| Toxicity/Toxicokinetics |
Stepronin is an expectorant and mucolytic agent with a well-characterized mechanism of action. As with any drug, potential toxicity may include effects on the respiratory and gastrointestinal systems. The compound's safety profile should be evaluated in preclinical toxicology studies. Stepronin is for research use only and is not approved for human therapeutic use. It represents a valuable tool compound for studying airway secretion and mucus clearance.
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| References | |
| Additional Infomation |
Stepronin is an N-acyl amino acid. Stepronin is an expectorant. Expectorants are any medications that can dissolve thick sputum and are commonly used to relieve shortness of breath. The viscosity of pulmonary mucus depends on the concentration of mucin and the presence of disulfide bonds between these macromolecules and DNA. Drug Indications Stepronin is an expectorant. Mechanism of Action Expectorants increase bronchial secretions, and by doing so, they help to thin thick bronchial secretions. Expectorants reduce the viscosity of bronchial secretions, thereby increasing mucus flow and making it easier to expel through coughing. Expectorants also break down the chemical structure of mucus molecules. The mucus becomes thinner and easier to expel through coughing. Pharmacodynamics This drug promotes the expulsion of pulmonary mucus by thinning mucus and lubricating the irritated airways.
Stepronin (CAS# 72324-18-6) is an orally active expectorant, although inhalation administration is preferable. It inhibits airway secretion in vitro by reducing Cl- secretion from epithelial cells and mucus glycoprotein secretion from submucosal glands. Stepronin is a synthetic N-acyl-alpha amino acid classified as a mucolytic and expectorant agent. It primarily targets airway epithelial cells to facilitate mucus clearance. The compound is for research use only and is not approved for human therapeutic use. |
| Molecular Formula |
C10H11NO4S2
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| Molecular Weight |
273.32864
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| Exact Mass |
273.013
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| CAS # |
72324-18-6
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| Related CAS # |
78126-10-0 (sodium);72324-18-6 (free acid);113790-28-6 (lysine salt);
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| PubChem CID |
54120
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| Appearance |
White to off-white solid powder
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| Density |
1.428 g/cm3
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| Boiling Point |
521.2ºC at 760 mmHg
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| Melting Point |
168-170ºC
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| Flash Point |
269ºC
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| Index of Refraction |
1.609
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| LogP |
1.601
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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 |
6
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| Heavy Atom Count |
17
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| Complexity |
321
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| Defined Atom Stereocenter Count |
0
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| SMILES |
OC(CNC(C(SC(C1=CC=CS1)=O)C)=O)=O
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| InChi Key |
JNYSEDHQJCOWQU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H11NO4S2/c1-6(9(14)11-5-8(12)13)17-10(15)7-3-2-4-16-7/h2-4,6H,5H2,1H3,(H,11,14)(H,12,13)
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| Chemical Name |
2-[2-(thiophene-2-carbonylsulfanyl)propanoylamino]acetic acid
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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) |
DMSO : ≥ 250 mg/mL (~914.65 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6586 mL | 18.2929 mL | 36.5858 mL | |
| 5 mM | 0.7317 mL | 3.6586 mL | 7.3172 mL | |
| 10 mM | 0.3659 mL | 1.8293 mL | 3.6586 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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