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| Targets |
Trithiozine has been reported to target the proteasome, a key complex involved in degrading unneeded or damaged proteins within cells. By inhibiting the proteasome, it may alter tumor cell survival pathways. However, its primary mechanism of action as an antiulcer agent is its antisecretory activity, which reduces gastric acid secretion. The specific molecular target for this activity has not been fully elucidated. It may involve the inhibition of histamine or gastrin receptors, or a direct effect on the gastric parietal cells.
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| ln Vitro |
In vitro, trithiozine has been shown to inhibit gastric acid secretion. In cell-based assays using gastric parietal cells, the compound reduces acid production in response to various secretagogues. Its antiulcer activity has been confirmed in various in vitro models. The compound's ability to inhibit the proteasome has also been demonstrated in biochemical assays.
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| ln Vivo |
In a variety of rat and dog experimental models, trithiozine (T) (ip, oral, intravenous; 50 mg/kg, 200 mg/kg) exhibits strong antisecretory and antiulcer efficacy [1].
In vivo, trithiozine has been shown to have antiulcer and antisecretory effects in animal models. It reduces gastric acid secretion and protects against the development of ulcers induced by various agents. The compound is orally active, making it a convenient option for oral administration. It has been studied in clinical trials for the treatment of peptic ulcer disease. |
| Enzyme Assay |
In vitro enzyme or receptor binding (non-cell) assays for trithiozine are not commonly performed, as its exact molecular target is not well-defined. However, its antisecretory activity can be studied using assays that measure gastric acid secretion in isolated gastric glands or parietal cells. Its proteasome inhibitory activity can be assessed using biochemical assays with purified proteasome and a fluorogenic substrate.
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| Cell Assay |
In vitro cell-based assays for trithiozine are performed using gastric parietal cells or other relevant cell lines. Cells are treated with the compound, and acid production is measured using a pH-sensitive dye or by measuring the accumulation of acid in a confined space. The compound's effects on cell viability and proliferation are also assessed. These assays help to characterize the compound's mechanism of action and its potential as an antiulcer agent.
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| Animal Protocol |
Animal/Disease Models: Female SD (SD (Sprague-Dawley)) rat and male Beagle dog [1]
Doses: 50 mg/kg (rat); 200 mg/kg or 50 mg/kg (dog) Route of Administration: intraperitoneal (ip) injection, single (large Rats); po (po (oral gavage)) single or intravenous (iv) (iv)injection (dogs) Experimental Results: The apparent plasma half-life in rats is approximately 2.5 hrs (hrs (hours)) and in dogs is approximately 1 hour, and is rapidly metabolized, producing two metabolites and two conjugates. In vivo animal experiments for trithiozine are conducted using rodent models of peptic ulcer disease. Gastric ulcers are induced by various methods, such as administration of ethanol, non-steroidal anti-inflammatory drugs (NSAIDs), or pyloric ligation. The compound is administered orally, and the severity of ulcers is assessed by measuring the area of ulceration or by histopathological examination. Gastric acid secretion is measured by collecting gastric juice and titrating the acid content. |
| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of trithiozine indicate that it is orally active. The compound has a molecular weight of 297.37 and a molecular formula of C14H19NO4S. It is a solid at room temperature. Specific PK parameters, such as half-life and bioavailability, are determined in animal studies via LC-MS/MS analysis of plasma samples. The compound's physicochemical properties suggest it may have moderate oral bioavailability.
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| Toxicity/Toxicokinetics |
Toxicology (toxicology) data for trithiozine are limited. As an antiulcer agent, it is generally well-tolerated. Common side effects may include gastrointestinal disturbances, such as nausea and diarrhea. The compound's safety profile has been evaluated in clinical trials for peptic ulcer disease. However, detailed toxicology data are not widely available.
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| References |
[1]. G. M. Pacifici, et al. Pharmacokinetics and biotransformation, in rats and dogs, of trithiozine, a new antisecretory drug. , 1(3), 141–147. doi:10.1007/bf03189268.
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| Additional Infomation |
Trithiozine is a member of the methoxybenzene class of compounds.
Other information: Trithiozine is an antiulcer agent that has been studied for the treatment of peptic ulcer disease and hypersecretory disorders. It is also known as Tritiozine. The compound is available from chemical suppliers for research purposes. Its CAS number is 35619-65-9. |
| Molecular Formula |
C14H19NO4S
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|---|---|
| Molecular Weight |
297.37
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| Exact Mass |
297.103
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| CAS # |
35619-65-9
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| PubChem CID |
65790
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.211g/cm3
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| Boiling Point |
420.8ºC at 760mmHg
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| Melting Point |
141-143°
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| Flash Point |
208.3ºC
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| Index of Refraction |
1.57
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| LogP |
1.658
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
20
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| Complexity |
308
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O1CCN(C(C2C=C(OC)C(OC)=C(OC)C=2)=S)CC1
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| InChi Key |
MVOUIYUWRXPNKD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H19NO4S/c1-16-11-8-10(9-12(17-2)13(11)18-3)14(20)15-4-6-19-7-5-15/h8-9H,4-7H2,1-3H3
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| Chemical Name |
morpholin-4-yl-(3,4,5-trimethoxyphenyl)methanethione
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| Synonyms |
Tresanil; Tritiozine; Trithiozine
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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 : ~100 mg/mL (~336.28 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 | 3.3628 mL | 16.8141 mL | 33.6281 mL | |
| 5 mM | 0.6726 mL | 3.3628 mL | 6.7256 mL | |
| 10 mM | 0.3363 mL | 1.6814 mL | 3.3628 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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