Tegoprazan
Based on 2 publication(s) in Google Scholar
Tegoprazan (CJ-12420), a potassium-competitive acid blocker, is a reversible, orally active and highly selective inhibitor of gastric H+/K+-ATPase. Tegoprazan inhibits gastric acid secretion and motility against porcine, canine and human H+/K+-ATPase with IC50 values ranging from 0.29-0.52 μM in vitro. Tegoprazan significantly improves colitis and enhances the intestinal epithelial barrier function in mice. Tegoprazan is promising for research of Inflammatory bowel, gastric acid-related, motilityimpaired diseases.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.71%
- CAS 番号: 942195-55-3
- 分子式: C20H19F2N3O3
- 分子量:387.38
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 Tegoprazan
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生物活性
IC50: 0.29-0.52 μM (H+/K+-ATPase)[1].
Tegoprazan (1.0 mM and 3.0 mM, 4 h) reduces dextran sulphate sodium (DSS)-induced colitis by maintaining high junction integrity of the epithelial mucosa in Caco-2 cells. Additionally, Tegoprazan protects the intestinal epithelial tight junction barrier and inhibits the increase in intestinal permeability in Caco-2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Caco-2 cells
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Concentration:1.0 mM and 3.0 mM
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Incubation Time:4 h
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Result:Increased the mRNA levels of Zo1 and Occludin combined with DSS compared to the DSS+Veh group in Caco-2 cells.
Tegoprazan (0.1, 1 and 10 mg/kg, p.o., a single day or daily for 5 days) exerts an antiulcer effect in Naproxen (HY-15030)-induced acute gastric ulcer rat model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Naproxen-induced acute gastric ulcer rat model[2].
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Dosage:0.1, 1 and 10 mg/kg
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Administration:p.o., a single day or daily for 5 days
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Result:Exerted an antiulcer effect in a dose-dependent manner and was effective at a single dose in naproxen-induced acute gastric ulcer rat model.
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Animal Model:DNBS and Tegoprazan-induced rats[2].
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Dosage:30 mg/kg
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Administration:p.o., twice daily for 5 days
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Result:Reduced mRNA expression levels of proinflammatory cytokines, especially interleukin-17 (IL17) in DNBS and Tegoprazan-induced rats.
化学情報
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CAS 番号 942195-55-3
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性状 Solid
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分子量 387.38
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分子式 C20H19F2N3O3
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Color Off-white to light yellow
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SMILES
FC1=CC(F)=C2[C@@H](OC3=CC(C(N(C)C)=O)=CC4=C3N=C(C)N4)CCOC2=C1
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別名
CJ-12420; RQ-00000004
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Int J Mol Sci
Anti-Inflammatory Effects of Tegoprazan in Lipopolysaccharide-Stimulated Bone-Marrow-Derived Macrophages. [Abstract]2023 Sep 26;24(19):14589. PMID: 37834036 -
J Pharm Biomed Anal
2023 May 10:228:115323. PMID: 36921447
溶剤 & 溶解度
DMSO : 100 mg/mL (258.14 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.45 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.45 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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取扱説明書 (2659 KB)
参考文献
[1]. Son M, et al. Novel Potassium-Competitive Acid Blocker, Tegoprazan, Protects Against Colitis by Improving Gut Barrier Function[J]. Front Immunol. 2022 May 25;13:870817. [Content Brief]
[2]. Kim DK, et al. Effects of Tegoprazan, a Novel Potassium-Competitive Acid Blocker, on Rat Models of Gastric Acid-Related Disease[J]. J Pharmacol Exp Ther. 2019 Jun;369(3):318-327. [Content Brief]
[3]. Takahashi N, et al. Tegoprazan, a Novel Potassium-Competitive Acid Blocker to Control Gastric Acid Secretion and Motility. J Pharmacol Exp Ther. 2018 Feb;364(2):275-286. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5814 mL | 12.9072 mL | 25.8144 mL | 64.5361 mL |
| 5 mM | 0.5163 mL | 2.5814 mL | 5.1629 mL | 12.9072 mL | |
| 10 mM | 0.2581 mL | 1.2907 mL | 2.5814 mL | 6.4536 mL | |
| 15 mM | 0.1721 mL | 0.8605 mL | 1.7210 mL | 4.3024 mL | |
| 20 mM | 0.1291 mL | 0.6454 mL | 1.2907 mL | 3.2268 mL | |
| 25 mM | 0.1033 mL | 0.5163 mL | 1.0326 mL | 2.5814 mL | |
| 30 mM | 0.0860 mL | 0.4302 mL | 0.8605 mL | 2.1512 mL | |
| 40 mM | 0.0645 mL | 0.3227 mL | 0.6454 mL | 1.6134 mL | |
| 50 mM | 0.0516 mL | 0.2581 mL | 0.5163 mL | 1.2907 mL | |
| 60 mM | 0.0430 mL | 0.2151 mL | 0.4302 mL | 1.0756 mL | |
| 80 mM | 0.0323 mL | 0.1613 mL | 0.3227 mL | 0.8067 mL | |
| 100 mM | 0.0258 mL | 0.1291 mL | 0.2581 mL | 0.6454 mL |
Tegoprazan 関連分類
HY-17623 関連分類
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