Vonoprazan Fumarate
Based on 6 publication(s) in Google Scholar
Vonoprazan Fumarate (TAK-438), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan Fumarate inhibits H+,K+-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan Fumarate is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease.
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- Pureza: 101.1%
- No. CAS: 881681-01-2
- Fòrmula: C21H20FN3O6S
- Peso molecular:461.46
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Almacenamiento:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Vonoprazan Fumarate
More- Int J Nanomedicine. 2025 Jun 24:20:8063-8083. [Abstract]
- Eur J Med Chem. 2024 Dec 5:279:116842. [Abstract]
- Drug Dev Res. 2022 Dec 9. [Abstract]
- Drug Metab Dispos. 2016 Oct;44(10):1543-9. [Abstract]
- Toxicol Appl Pharmacol. 2024 May:486:116945. [Abstract]
- Br J Clin Pharmacol. 2019 Jul;85(7):1454-1463. [Abstract]
Actividad biológica
IC50: 19 nM (porcine gastric H+,K+-ATPase, at pH 6.5)[2]
Vonoprazan (0.1 nM-10 μM; 30 minutes) exhibits porcine gastric H+ ,K+-ATPase activity in a concentration-dependent manner[2].
Vonoprazan does not inhibit Na+,K+-ATPase activity, even at concentrations 500 times higher than their IC50 values against gastric H+,K+-ATPase activity[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male 7- or 8-week-old Sprague-Dawley rat[2]
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Dosage:0.5, 1, 2, and 4 mg/kg
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Administration:Oral administration
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Result:Inhibited basal gastric acid secretion in a dose-dependent manner.
Chemical Information
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No. CAS 881681-01-2
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Appearance Solid
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Peso molecular 461.46
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Fòrmula C21H20FN3O6S
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Color White to off-white
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SMILES
O=C(O)/C=C/C(O)=O.O=S(N1C=C(CNC)C=C1C2=CC=CC=C2F)(C3=CC=CN=C3)=O
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Synonyms
TAK-438
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (6)
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Journal Impact Factor
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Most Recent
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Int J Nanomedicine
Macrophage Membrane-Coated Liposomes Delivering Vonoprazan Disrupt Mitochondrial Oxidative Phosphorylation in Diffuse Large B-Cell Lymphoma. [Abstract]2025 Jun 24:20:8063-8083. PMID: 40626139 -
Eur J Med Chem
2024 Dec 5:279:116842. PMID: 39260319 -
Drug Dev Res
Differential effects of proton pump inhibitors and vonoprazan on vascular endothelial growth factor expression in cancer cells. [Abstract]2022 Dec 9. PMID: 36484282 -
Drug Metab Dispos
Lansoprazole Exacerbates Pemetrexed-Mediated Hematologic Toxicity by Competitive Inhibition of Renal Basolateral Human Organic Anion Transporter 3. [Abstract]2016 Oct;44(10):1543-9. PMID: 27465369 -
Toxicol Appl Pharmacol
In silico and in vitro assessment of drugs potentially causing adverse effects by inhibiting CYP17A1. [Abstract]2024 May:486:116945. PMID: 38688424 -
Br J Clin Pharmacol
Effects of proton pump inhibitors, esomeprazole and vonoprazan, on the disposition of proguanil, a CYP2C19 substrate, in healthy volunteers. [Abstract]2019 Jul;85(7):1454-1463. PMID: 30845361
Solvente y solubilidad
DMSO : 50 mg/mL (108.35 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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (5.42 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 (5.42 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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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.
Pureza y Documentación
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Ficha de datos (275 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)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Arikawa Y, et al. Discovery of a novel pyrrole derivative 1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine fumarate (TAK-438) as a potassium-competitive acid blocker (P-CAB). J Med Chem, 2012, 55(9), 4446-4456. [Content Brief]
[2]. Hori Y, et al. 1-[5-(2-Fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine monofumarate (TAK-438), a novel and potent potassium-competitive acid blocker for the treatment of acid-related diseases. J Pharmacol Exp Ther, 2010, 335(1), 231-238. [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 (sealed storage, away from moisture and light). 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 | 2.1670 mL | 10.8352 mL | 21.6704 mL | 54.1759 mL |
| 5 mM | 0.4334 mL | 2.1670 mL | 4.3341 mL | 10.8352 mL | |
| 10 mM | 0.2167 mL | 1.0835 mL | 2.1670 mL | 5.4176 mL | |
| 15 mM | 0.1445 mL | 0.7223 mL | 1.4447 mL | 3.6117 mL | |
| 20 mM | 0.1084 mL | 0.5418 mL | 1.0835 mL | 2.7088 mL | |
| 25 mM | 0.0867 mL | 0.4334 mL | 0.8668 mL | 2.1670 mL | |
| 30 mM | 0.0722 mL | 0.3612 mL | 0.7223 mL | 1.8059 mL | |
| 40 mM | 0.0542 mL | 0.2709 mL | 0.5418 mL | 1.3544 mL | |
| 50 mM | 0.0433 mL | 0.2167 mL | 0.4334 mL | 1.0835 mL | |
| 60 mM | 0.0361 mL | 0.1806 mL | 0.3612 mL | 0.9029 mL | |
| 80 mM | 0.0271 mL | 0.1354 mL | 0.2709 mL | 0.6772 mL | |
| 100 mM | 0.0217 mL | 0.1084 mL | 0.2167 mL | 0.5418 mL |
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