| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 100mg |
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| Other Sizes |
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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].
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| References | |
| Additional Infomation |
Pumaprazole is an imidazo-pyridine derivative with reversibly binding acid pump antagonist (APA) activity. Contrary to the mechanism of action of the proton pump inhibitors, which need to be activated by acid within the parietal cell canaliculus and which covalently react through the action of an active intermediate with the SH groups of the H+/K+-ATPase proton pump, pumaprazole competes reversibly with potassium binding on the extracytoplasmic face of the catalytic (alpha) subunit of the proton pump, immediately interrupting the pump's activity and the parietal cell secretion of H+ ions into the gastric lumen, the final step in gastric acid production.
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| 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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