Tenatoprazole
Tenatoprazole
CAS: 113712-98-4
Molecular Formula: C16H18N4O3S
Tenatoprazole - Names and Identifiers
Tenatoprazole - Physico-chemical Properties
| Molecular Formula | C16H18N4O3S |
| Molar Mass | 346.4 |
| Density | 1.43±0.1 g/cm3(Predicted) |
| Melting Point | 178-180°C |
| Boling Point | 570.4±60.0 °C(Predicted) |
| Flash Point | 311.5°C |
| Solubility | DMSO (Slightly, Heated), Methanol (Slightly, Heated) |
| Vapor Presure | 5.8E-14mmHg at 25°C |
| Appearance | Solid |
| Color | Off-White to Light Pink |
| pKa | 4.61±0.40(Predicted) |
| Storage Condition | Sealed in dry,2-8°C |
| Stability | Hygroscopic, Temperature Sensitive |
| Refractive Index | 1.673 |
| Use | Drugs for digestive system |
| In vitro study | As with other proton pump inhibitors that have been discovered, Tenatoprazole-labeled only the α-subunit of the gastric H +,K +-ATPase, about 2.6 nmol/mg binds to H +,K +-ATP enzyme. The two enantiomers,(R)-or (S)-tenatoprazole, combined with the same stoichiometry, resulted in 88% inhibition. Tenatoprazole tracks only polypeptides containing the fifth and sixth transmembrane fragments, which contain two cysteines, the cysteine 813 of the luminal vestibule and the cysteine 822 of the sixth transmembrane domain. |
| In vivo study | The prediction of chemical activation in fasting rats showed that Tenatoprazole was slowly activated in vivo. Although there is gastric acid secretion in fasting rats, Tenatoprazole inhibits the enzyme activity by about 20-30%. (S)-tenatoprazole sodium salt hydrate provided higher C max,T max, and ACC in dogs of 183 ng/mL,1.3 h, and 822 ng * h/mL, respectively. |
Tenatoprazole - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | R22 - Harmful if swallowed R36/37/38 - Irritating to eyes, respiratory system and skin. |
| Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36/37 - Wear suitable protective clothing and gloves. |
Tenatoprazole - Reference Information
| anti-ulcer drug | tenozole (tenatoprazole) is a new proton pump inhibitor, which is jointly developed by Tokyo Tanabe Company, Japan Mitsubishi Company and Japan Hokuriku Pharmaceutical Company, and has passed Phase II clinical trials. It can act on gastric mucosal parietal cells, reduce H /K-ATPase activity in parietal cells, inhibit gastric acid secretion, and has antibacterial activity against Helicobacter pylori. It is mainly used to treat gastric ulcers, duodenal ulcers, and reflux Esophagitis and Zhuo-Ai syndrome are diseases related to gastric acid secretion disorders. Compared with the same type of drugs, Tatoprazole inhibits the activity of H /K-ATPase and has higher stability, and its curative effect is 7 times stronger than the similar product omeprazole widely used in clinical practice. The drug has not been marketed in China and has not been approved for production, which has broad market prospects and development potential. Proton pump inhibitors (proton pump inhibitors) are used to treat acid-related diseases and are widely used clinically and have good curative effects in the past ten years. It can quickly pass through the cell membrane of the gastric wall, gather in the strongly acidic secretory tubule, and covalently combine with the sulfhydryl group of H /K-ATPase (proton pump) to form a disulfide bond, inactivate the proton pump and inhibit the enzyme H /K transport, so as to achieve the effect of acid suppression. Compared with the H2 receptor antagonist, a drug used in clinical practice, proton pump inhibitors have different action sites and have different characteristics, that is, good acid suppression at night, fast onset, strong acid suppression and long time, Easy to take, these drugs can efficiently and quickly inhibit gastric acid secretion and remove Helicobacter pylori, and are widely used in the treatment of gastric ulcer, duodenal ulcer, reflux esophagitis and Zhuo-Ai syndrome. At present, the main proton pump inhibitors on the market are omeprazole, lansoprazole, pantoprazole, rabeprazole and esomeprazole. |
| physical and chemical properties | this product is white or white-like crystalline powder with a melting point of 174~175 ℃. Soluble in chloroform, insoluble in alcohol and water. Compared with other proton pump inhibitors, this product has stable chemical properties. The stability of 34 omeprazole preparations from 13 countries including Portugal, Brazil, India and China has been determined in China. The results showed that only 6 products (18%) showed good physical and chemical stability during the test. 27 products (79%) are poor (including Chinese products), their active ingredients have obvious chemical decomposition, and their physical properties such as color and dissolution have also changed accordingly. The results of a test aimed at comparing the stability of various proton pump inhibitors showed that after 8 days of investigation under the conditions of 60°C and 75% relative humidity, only 3% of the active ingredients were left after the decomposition of omeprazole. The data of Tatoprazole is 77%, indicating that the stability of Tatoprazole is far better than Omeprazole, and it is the most potential product of its kind that has been developed. (2016-02-01) |
| synthetic route | from 2-mercapto-5-methoxyimidazolo [4,5-b] pyridine (2) and 2-chloromethyl-3, 5-dimethyl-4-methoxypyridine hydrochloride (3) is synthesized by nucleophilic substitution 2-(4-methoxy-3, 5-Dimethylpyridine-2-methylthio)-5-methoxyimidazo [4,5-b] pyridine (4), 4 is oxidized to give 1. Fig. 1 shows the synthetic route of tenozole |
| Biological activity | Tenatoprazole (TU-199) is a proton pump inhibitor prodrug that inhibits proton transport. The IC50 is 3.2 μM. Tenatoprazole only labeled the α-subunit of the stomach H (+),K (+)-ATPase, about 2.6 nM/mg bound to H (+),K (+)-ATPase. |
| Target | Value |
| Proton pump () | |
| H(+),K(+)-ATPase (Cell-free assay) | 3.2 μM |
| use | is used to treat gastric ulcer, duodenal ulcer, reflux esophagitis, Zhuo-Ai syndrome and other diseases related to gastric acid secretion disorders. Medicines for digestive system |
Last Update：2024-04-09 21:11:58
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