Size | Price | Stock | Qty |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Targets |
IC50: 19 nM (porcine gastric H+,K+-ATPase, at pH 6.5)[2]
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ln Vitro |
Porcine stomach H+,K+-ATPase activity is seen in response to vonoprazan (0.1 nM–10 μM; 30 minutes) in a concentration-dependent manner[2]. Even at 500 times higher concentrations than their IC50 values against stomach H+,K+-ATPase activity, vonoprazan does not inhibit Na+,K+-ATPase activity[2].
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ln Vivo |
Rats' baseline and 2-deoxy-D-glucose (2DG, 200 mg/kg sc)-stimulated stomach acid production is totally inhibited by vonoprazan (1-4 mg/kg; po) at a dose of 4 mg/kg[2].
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Animal Protocol |
Animal/Disease Models: Male 7- or 8weeks old SD (Sprague-Dawley) rat[2]
Doses: 0.5, 1, 2, and 4 mg/kg Route of Administration: Oral administration Experimental Results: Inhibited basal gastric acid secretion in a dose-dependent manner. |
References |
[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.
[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), |
Molecular Formula |
C21H20FN3O6S
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Molecular Weight |
461.46
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CAS # |
881681-01-2
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Related CAS # |
Vonoprazan;881681-00-1;Vonoprazan hydrochloride;1957202-44-6
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
C(/C(=O)O)=C\C(=O)O.S(C1C=NC=CC=1)(N1C=C(CNC)C=C1C1C=CC=CC=1F)(=O)=O
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
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: 50 mg/mL (108.35 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.42 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 25.0 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: ≥ 2.5 mg/mL (5.42 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 25.0 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: ≥ 2.5 mg/mL (5.42 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 | 2.1670 mL | 10.8352 mL | 21.6704 mL | |
5 mM | 0.4334 mL | 2.1670 mL | 4.3341 mL | |
10 mM | 0.2167 mL | 1.0835 mL | 2.1670 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.