| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Pumaprazole's primary target is the gastric H+/K+-ATPase (the proton pump). It acts as a reversible antagonist by competing with potassium binding on the extracytoplasmic face of the catalytic (alpha) subunit of the proton pump. This immediately interrupts the pump's activity and the parietal cell secretion of H+ ions.
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| ln Vitro |
In vitro, Pumaprazole acts as a reversible proton pump antagonist. Its activity is characterized by its ability to inhibit the H+/K+-ATPase enzyme in a reversible manner, distinguishing it from irreversible PPIs.
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| ln Vivo |
Pramazole is an antagonist of the reversible proton pump. Pramarazole more effectively than ranitidine suppresses baseline acid secretion in Ghosh-Schild rats. Pumalazole demonstrated efficacy in a repeated-dose study in this animal on days 1 (11 μmol/kg, 95% confidence limits 5 and 23) and 7 (10 μmol/kg, 95% confidence limits 4 and 23). displays the identical ID50 value. Pumalazole's greater dose (54 μmol/kg) prolongs the pH-raising impact, whereas the lesser dose (27 μmol/kg) can quickly raise the luminal pH to almost neutrality [1].
In vivo, Pumaprazole suppresses baseline acid secretion more effectively than ranitidine in Ghosh-Schild rats. This demonstrates its potential as a potent acid-suppressing agent. Its reversible mechanism of action may offer advantages over irreversible PPIs in terms of faster onset and offset of action. |
| Enzyme Assay |
The in vitro activity of Pumaprazole is assessed using cell-free H+/K+-ATPase enzyme assays. The enzyme is incubated with its substrates (ATP and K+) in the presence of varying concentrations of Pumaprazole. The inhibition of ATP hydrolysis is measured to determine the compound's potency.
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| Cell Assay |
For cellular assays, gastric parietal cells are used to study the effects of Pumaprazole on acid secretion. Cells are cultured in appropriate media and treated with various concentrations of the compound. The inhibition of acid production is measured to assess its efficacy.
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| Animal Protocol |
In vivo, Pumaprazole is typically administered orally to animal models, such as Ghosh-Schild rats. The compound's effect on gastric acid secretion is assessed by measuring the pH of gastric contents or by using more sophisticated techniques to quantify acid output.
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| ADME/Pharmacokinetics |
Pumaprazole has a molecular weight of 338.40 g/mol and a molecular formula of C19H22N4O2. Its IUPAC name is methyl N-[2-[[(2,3-dimethylimidazo[1,2-a]pyridin-8-yl)amino]methyl]-3-methylphenyl]carbamate. It is soluble in DMSO.
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| Toxicity/Toxicokinetics |
Specific toxicity data for Pumaprazole is not detailed in the provided search results. As a research compound, its safety profile has not been fully established. Its mechanism of action as a proton pump antagonist suggests it may have effects on gastric acid secretion and related physiological processes.
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| References | |
| Additional Infomation |
Promaprozil is an imidazopyridine derivative with reversible acid pump antagonist (APA) activity. Unlike proton pump inhibitors, which require acid activation within the parietal cell tubules and covalently react with the sulfhydryl (-SH) group of the H+/K+-ATPase proton pump via an active intermediate, promaprozil reversibly competes with potassium ions on the extracellular side of the proton pump catalytic subunit (α subunit), thereby immediately blocking proton pump activity and inhibiting the secretion of H+ ions into the gastric lumen by parietal cells—the final step in gastric acid production.
Pumaprazole is a research compound that was developed as a reversible proton pump antagonist. Its reversible mechanism of action distinguishes it from conventional PPIs and makes it a valuable tool for studying gastric acid secretion. It is not approved for clinical use. |
| Molecular Formula |
C19H22N4O2
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|---|---|
| Molecular Weight |
338.411
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| Exact Mass |
338.174
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| CAS # |
158364-59-1
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| PubChem CID |
3052764
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.21g/cm3
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| Index of Refraction |
1.615
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| LogP |
4.136
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
25
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| Complexity |
461
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NZQTVUWEPPDOKK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H22N4O2/c1-12-7-5-8-16(22-19(24)25-4)15(12)11-20-17-9-6-10-23-14(3)13(2)21-18(17)23/h5-10,20H,11H2,1-4H3,(H,22,24)
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| Chemical Name |
methyl N-[2-[[(2,3-dimethylimidazo[1,2-a]pyridin-8-yl)amino]methyl]-3-methylphenyl]carbamate
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| Synonyms |
BY841; BY 841; BY-841
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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 (~295.51 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.39 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 (7.39 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9550 mL | 14.7750 mL | 29.5500 mL | |
| 5 mM | 0.5910 mL | 2.9550 mL | 5.9100 mL | |
| 10 mM | 0.2955 mL | 1.4775 mL | 2.9550 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.
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