Tenatoprazole
Based on 1 Customer Validation
Tenatoprazole (TU-199) is an orally active imidazopyridine-based proton pump inhibitor with a prolonged plasma half-life. Tenatoprazole inhibits hog gastric H+/K+-ATPase activity with an IC50 of 6.2 μM. Tenatoprazole blocks the interaction of ubiquitin with the ESCRT-1 factor Tsg101, inhibits production of several enveloped viruses, including EBV.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.79%
- CAS. Nr.: 113712-98-4
- Formel: C16H18N4O3S
- Molecular Weight:346.40
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
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| HEK-293T | IC50 |
>100 μM
Compound: Tenatoprazole
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Inhibition of mouse Ido1 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis
Inhibition of mouse Ido1 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis
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[PMID: 23122865] |
| HEK-293T | IC50 |
1.8 μM
Compound: Tenatoprazole
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Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis
Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis
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[PMID: 23122865] |
| HEK-293T | IC50 |
20 μM
Compound: Tenatoprazole
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Inhibition of recombinant human C-MYC/DDK-tagged ENGase expressed in HEK293T cells using heat inactivated bovine ribonuclease B as substrate pretreated for 15 mins followed by substrate addition after 90 mins by SDS-PAGE analysis
Inhibition of recombinant human C-MYC/DDK-tagged ENGase expressed in HEK293T cells using heat inactivated bovine ribonuclease B as substrate pretreated for 15 mins followed by substrate addition after 90 mins by SDS-PAGE analysis
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[PMID: 28512024] |
| HepG2 | IC50 |
>10 μM
Compound: 92309022
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HARVARD: Cytotoxicity in HepG2 cell line
HARVARD: Cytotoxicity in HepG2 cell line
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[PMID: 22586124] |
| HepG2 | IC50 |
0.224 μM
Compound: 92309022
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HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells
HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells
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[PMID: 22586124] |
Tenatoprazole (TU-199) (0.1, 0.2, 0.4 mg/kg; oral; single; Heidenhain-pouch dogs) dose-dependently suppresses gastric acid secretion stimulated by histamine infusion[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 113712-98-4
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Appearance Solid
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Molecular Weight 346.40
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Formel C16H18N4O3S
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Color White to pink
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SMILES
O=S(C1=NC2=CC=C(OC)N=C2N1)CC3=NC=C(C)C(OC)=C3C
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Synonyms
TU-199
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 50 mg/mL (144.34 mM; ultrasonic and warming and heat to 60°C; 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (7.22 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 (7.22 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
Reinheit & Dokumentation
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Data Sheet (272 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Thomson AB, et al. Comparison of the effects of fasting morning, fasting evening and fed bedtime administration of tenatoprazole on intragastric pH in healthy volunteers: a randomized three-way crossover study. Aliment Pharmacol Ther. 2006;23(8):1179-1187. [Content Brief]
[2]. Uchiyama K, et al. Effects of TU-199, a novel H+, K(+)-ATPase inhibitor, on gastric acid secretion and gastroduodenal ulcers in rats. Methods Find Exp Clin Pharmacol. 1999;21(2):115-122. [Content Brief]
[3]. Mannemuddhu SS, et al. Prazoles Targeting Tsg101 Inhibit Release of Epstein-Barr Virus following Reactivation from Latency. J Virol. 2021;95(13):e0246620. [Content Brief]
[4]. Uchiyama K, et al. The long-lasting effect of TU-199, a novel H+, K(+)-ATPase inhibitor, on gastric acid secretion in dogs. J Pharm Pharmacol. 1999;51(4):457-464. [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 | 2.8868 mL | 14.4342 mL | 28.8684 mL | 72.1709 mL |
| 5 mM | 0.5774 mL | 2.8868 mL | 5.7737 mL | 14.4342 mL | |
| 10 mM | 0.2887 mL | 1.4434 mL | 2.8868 mL | 7.2171 mL | |
| 15 mM | 0.1925 mL | 0.9623 mL | 1.9246 mL | 4.8114 mL | |
| 20 mM | 0.1443 mL | 0.7217 mL | 1.4434 mL | 3.6085 mL | |
| 25 mM | 0.1155 mL | 0.5774 mL | 1.1547 mL | 2.8868 mL | |
| 30 mM | 0.0962 mL | 0.4811 mL | 0.9623 mL | 2.4057 mL | |
| 40 mM | 0.0722 mL | 0.3609 mL | 0.7217 mL | 1.8043 mL | |
| 50 mM | 0.0577 mL | 0.2887 mL | 0.5774 mL | 1.4434 mL | |
| 60 mM | 0.0481 mL | 0.2406 mL | 0.4811 mL | 1.2028 mL | |
| 80 mM | 0.0361 mL | 0.1804 mL | 0.3609 mL | 0.9021 mL | |
| 100 mM | 0.0289 mL | 0.1443 mL | 0.2887 mL | 0.7217 mL |
Tenatoprazole Related Classifications
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