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100mg |
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250mg |
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500mg |
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1g |
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2g |
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5g |
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10g |
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Vonoprazan (TAK-438) is a novel, orally bioavailable and potent P-CAB (potassium-competitive acid blocker) that reversibly inhibits H+/K+, ATPase with IC50 of 19 nM (pH 6.5), controls gastric acid secretion. It was approved in the Japanese market in February 2015. In cultured gastric glands, TAK-438 treatment resulted in a longer and stronger acid formation inhibition. The inhibition effect of TAK-438 on acid secretion seemed to be associated with gastric parietal cell physiology.
ln Vitro |
Vonoprazan (0.1 nM-10 μM; 30 minutes) activates porcine gastric H+, K+-ATPase in a concentration-dependent manner [2]. Vonoprazan does not block Na+,K+-ATPase activity, even at doses 500 times greater than the IC50 values for gastric H+,K+-ATPase activity[2].
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ln Vivo |
Rats' baseline and 2-deoxy-D-glucose (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 mg/kg, 1 mg/kg, 2 mg/kg, 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), 231-238. [3]. Sugimoto M, et al. Role of Vonoprazan in Helicobacter pylori Eradication Therapy in Japan. Front Pharmacol. 2019 Jan 15;9:1560. |
Molecular Formula |
C17H16FN3O2S
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Molecular Weight |
345.3912
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CAS # |
881681-00-1
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Related CAS # |
Vonoprazan Fumarate;881681-01-2;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 |
S(C1=C([H])N=C([H])C([H])=C1[H])(N1C([H])=C(C([H])([H])N([H])C([H])([H])[H])C([H])=C1C1=C([H])C([H])=C([H])C([H])=C1F)(=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 |
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 : ~100 mg/mL (~289.53 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.24 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 (7.24 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 (7.24 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 | 2.8953 mL | 14.4764 mL | 28.9528 mL | |
5 mM | 0.5791 mL | 2.8953 mL | 5.7906 mL | |
10 mM | 0.2895 mL | 1.4476 mL | 2.8953 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.