| Size | Price | Stock | Qty |
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| 100mg |
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| 500mg |
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| Other Sizes |
| Targets |
Troxipide does not have a single well-defined molecular target but exerts its gastroprotective effects through multiple mechanisms. It is a non-antisecretory gastroprotective agent with antiulcer, anti-inflammatory and mucus-secreting properties irrespective of pH of stomach or duodenum. It promotes the repair of gastric ulcer sites, healing of chronic ulcers, protects the mucosa, increases gastric mucosal blood flow, activates gastric mucosal metabolism, normalizes gastric mucosal composition, and increases gastric mucosal mucopolysaccharide and prostaglandin content.
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| ln Vitro |
By increasing gastric mucosal blood flow and gastric mucosal defense factors, boosting tissue repair, blood circulation, metabolism, and GU healing, troxipide plays a unique inhibitory, therapeutic, and preventive role in the stomach [1].
In vitro, troxipide has been shown to have anti-inflammatory and mucus-secreting properties. It promotes mucus secretion in gastric epithelial cells. These in vitro activities are consistent with its mechanism of action as a gastric cytoprotective agent. It enhances defensive factors in the gastric mucosa. |
| ln Vivo |
The intravenous administration of troxipide (40 mg/kg) substantially improves gastric ulcers (GU) [1]. Troxipide (40 mg/kg; intravenously) had a half-life of 210 minutes in NCG rats and 428.73 minutes in GUG rats, respectively [1].
In vivo, troxipide has been shown to be effective in healing gastric ulcers and gastritis in clinical studies. It has been used for the treatment of gastroesophageal reflux disease, gastric ulcers, and for the amelioration of gastric mucosal lesions in acute and chronic gastritis. The compound is administered orally and is well-tolerated. Its mechanism of action is distinct from that of acid-suppressing drugs, such as proton pump inhibitors and H2 receptor antagonists. Troxipide is available in Japan for the treatment of gastritis and gastric ulcers. |
| Enzyme Assay |
In vitro enzyme or receptor binding (non-cell) assays for troxipide are not commonly performed, as it does not have a single specific target. However, its effects on gastric mucosal defense factors can be studied using biochemical assays. For example, its ability to stimulate mucin secretion can be assessed using assays that measure mucin production. Its anti-inflammatory effects can be studied by measuring the inhibition of inflammatory mediators.
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| Cell Assay |
In vitro cell-based assays for troxipide are performed using gastric epithelial cells. Cells are treated with the compound, and mucus production, cell viability, and the expression of cytoprotective genes are assessed. The compound's effects on inflammatory responses are measured by assessing the production of inflammatory cytokines. These assays help to characterize the compound's mechanism of action.
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| Animal Protocol |
Animal/Disease Models: normal control group (NCG) and gastric ulcer group (GUG) rats (5% acetic acid 10 mL/kg/day) [1]
Doses: 10, 20, 40, 60 mg/kg Route of Administration: oral; Daily; 2-week Experimental Results: Levels of these cytokines (IL-17, IL-6, TNF-α, IFN-γ, and AP-1) were Dramatically diminished, indicating significant remission of GU. Animal/Disease Models: NCG and GUG rats [1] Doses: intravenous (iv) (iv)injection 40 mg/kg Route of Administration: intravenous (iv) (iv)injection Experimental Results: T1/2 of NCG and GUG rats were 210 minutes and 428.73 minutes respectively. In vivo animal experiments for troxipide are conducted using rodent models of gastric ulcers. Gastric ulcers are induced by various methods, such as administration of ethanol, non-steroidal anti-inflammatory drugs (NSAIDs), or stress. The compound is administered orally, and the severity of ulcers is assessed by measuring the area of ulceration or by histopathological examination. The compound's effects on gastric mucosal blood flow, mucus production, and inflammatory cell infiltration are also assessed. |
| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of troxipide indicate that it is well-absorbed after oral administration. The compound has a molecular weight of 294.35 and a molecular formula of C15H22N2O4. It is a white to almost white powder. The compound is typically administered orally. Specific PK parameters, such as half-life and bioavailability, are determined in clinical studies via LC-MS/MS analysis of plasma samples. The compound is metabolized in the liver and excreted renally.
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| Toxicity/Toxicokinetics |
Toxicology (toxicology) data for troxipide indicate that it is generally well-tolerated. Common side effects are rare and may include mild gastrointestinal disturbances, such as constipation or diarrhea. The compound has a favorable safety profile, with no significant hepatotoxicity, nephrotoxicity, or other serious adverse effects reported at therapeutic doses. It is not genotoxic, carcinogenic, or teratogenic.
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| References |
[1]. Hongbin Guo, et al. Metabolites profiling and pharmacokinetics of troxipide and its pharmacodynamics in rats with gastric ulcer. Sci Rep. 2020 Aug 12;10(1):13619.
[2]. K Kusugami, et al. Troxipide, a novel antiulcer compound, has inhibitory effects on human neutrophil migration and activation induced by various stimulants. Dig Liver Dis. 2000 May;32(4):305-11. |
| Additional Infomation |
Trazopyridine belongs to the benzamide class of drugs.
Other information: Troxipide is a gastric cytoprotective agent used for the treatment of gastric ulcers, gastritis, and gastroesophageal reflux disease. It is a novel compound that does not inhibit acid secretion. The compound is also known as 3,4,5-trimethoxy-N-piperidin-3-ylbenzamide. Its CAS number is 30751-05-4. |
| Molecular Formula |
C15H22N2O4
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| Molecular Weight |
294.351
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| Exact Mass |
294.157
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| CAS # |
30751-05-4
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| PubChem CID |
5597
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
407.5±45.0 °C at 760 mmHg
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| Melting Point |
179-182ºC
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| Flash Point |
200.3±28.7 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.547
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| LogP |
0.24
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
21
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| Complexity |
326
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(NC1CNCCC1)C2=CC(OC)=C(OC)C(OC)=C2
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| InChi Key |
YSIITVVESCNIPR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H22N2O4/c1-19-12-7-10(8-13(20-2)14(12)21-3)15(18)17-11-5-4-6-16-9-11/h7-8,11,16H,4-6,9H2,1-3H3,(H,17,18)
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| Chemical Name |
3,4,5-trimethoxy-N-piperidin-3-ylbenzamide
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| Synonyms |
BRN 0493078; BRN-0493078; BRN0493078
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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 : ~9.09 mg/mL (~30.88 mM)
H2O : ~1 mg/mL (~3.40 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.91 mg/mL (3.09 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 9.1 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: ≥ 0.91 mg/mL (3.09 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 9.1 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. View More
Solubility in Formulation 3: ≥ 0.91 mg/mL (3.09 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3973 mL | 16.9866 mL | 33.9732 mL | |
| 5 mM | 0.6795 mL | 3.3973 mL | 6.7946 mL | |
| 10 mM | 0.3397 mL | 1.6987 mL | 3.3973 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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