| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
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Purity: ≥98%
Ilaprazole (IY81149) is an orally bioavailable anti-ulcer agent, acting as a proton pump inhibitor (PPI) and is used in the treatment of dyspepsia, peptic ulcer disease (PUD), gastroesophageal reflux disease (GORD/GERD) and duodenal ulcer. Clinical studies show that ilaprazole is at least as potent a PPI as omeprazole when taken in equivalent doses. Studies also showed that ilaprazole significantly prevented the development of reflux oesophagitis.
| ln Vitro |
When it comes to the buildup of 14C-aminopyrine in histamine-stimulated parietal cells, ilaprazole (IY-81149) sodium exhibits an IC50 of 9 nM [1].
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| ln Vivo |
Ilaprazole (3-30 mg/kg; id) dose-dependently reduces stomach acid secretion [1]. In anesthetized rats, ilaprazole dose-dependently increased gastric pH, whereas histamine infusion decreased gastric pH. In the case of intravenous injection, the ED50s of ilaprazole and omeprazole are 1.2 and 1.4 mg/kg, and in the case of id administration, the ED50s of ilaprazole and omeprazole are 3.9 and 4.1, respectively. mg/kg. Ilaprazole also significantly reduces pentagastrin-stimulated gastric secretion. When taken id, its ED50 is 2.1 mg/kg, whereas the ED50 of omeprazole is 3.5 mg/kg. When taken intravenously, ilaprazole is similar to omeprazole. Ilaprazole also strongly decreased stomach acid output in fistula rats. For intraduodenal administration, the ED50 of ilaprazole is 0.43 mg/kg and that of omeprazole is 0.68 mg/kg [1].
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| Animal Protocol |
Animal/Disease Models: Male SD rat (after pyloric ligation) [1]
Doses: 3, 10, 30 mg/kg Route of Administration: Intraduodenal Experimental Results: At 3 mg/kg, acid excretion and volume were Dramatically inhibited About 60% and 46%, respectively. At a concentration of 30 mg/kg, it inhibited acid excretion by 93% and volume by 73%, respectively. |
| References |
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| Additional Infomation |
Ilaprazole is a sulfoxide and a member of benzimidazoles.
Ilaprazole has been investigated in Helicobacter Infections. Ilaprazole is a substituted benzimidazole prodrug with selective and irreversible proton pump inhibitor activity. A weak base, ilaprazole accumulates in the acidic environment of the secretory canaliculus of the gastric parietal cell where it is converted to an active sulfenamide form that binds to cysteine sulfhydryl groups on the luminal aspect of the proton pump hydrogen-potassium adenosine triphosphatase (H+/K+ ATPase), thereby inhibiting the pump's activity and the parietal cell secretion of H+ ions into the gastric lumen, the final step in gastric acid production. |
| Molecular Formula |
C19H18N4O2S
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|---|---|
| Molecular Weight |
366.44
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| Exact Mass |
366.115
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| CAS # |
172152-36-2
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| Related CAS # |
Ilaprazole sodium;172152-50-0
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| PubChem CID |
214351
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| Appearance |
Off-white to gray solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
651.0±65.0 °C at 760 mmHg
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| Flash Point |
347.5±34.3 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
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| Index of Refraction |
1.710
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| LogP |
2.66
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
26
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| Complexity |
502
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
HRRXCXABAPSOCP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H18N4O2S/c1-13-17(20-8-7-18(13)25-2)12-26(24)19-21-15-6-5-14(11-16(15)22-19)23-9-3-4-10-23/h3-11H,12H2,1-2H3,(H,21,22)
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| Chemical Name |
1H-Benzimidazole,2-[[(4-methoxy-3-methyl-2-pyridinyl)methyl]sulfinyl]-5-(1H-pyrrol-1-yl)- (9CI)
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| Synonyms |
IY81149 IY-81149 IY 81149 Noltec.
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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: This product is not stable in solution, please use freshly prepared working solution for optimal results. |
| 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 : ≥ 35 mg/mL (~95.51 mM)
Ethanol : ~5 mg/mL (~13.64 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (3.41 mM) (saturation unknown) in 10% EtOH + 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 12.5 mg/mL clear EtOH 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: ≥ 1.25 mg/mL (3.41 mM) (saturation unknown) in 10% EtOH + 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 12.5 mg/mL clear EtOH 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: ≥ 1.25 mg/mL (3.41 mM) (saturation unknown) in 10% EtOH + 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 | 2.7290 mL | 13.6448 mL | 27.2896 mL | |
| 5 mM | 0.5458 mL | 2.7290 mL | 5.4579 mL | |
| 10 mM | 0.2729 mL | 1.3645 mL | 2.7290 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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