| 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 |
Purity: ≥98%
| Targets |
Ilaprazole targets the gastric H+/K+-ATPase (proton pump), which is the enzyme responsible for the final step in gastric acid secretion. By inhibiting this enzyme, Ilaprazole effectively blocks the production of gastric acid, making it useful for the treatment of acid-related disorders such as gastric ulcers, dyspepsia, and GERD. It has an IC50 of 6.0 μM for pump inhibitory activity.
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| 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].
Ilaprazole inhibits H+/K+-ATPase with an IC50 of 6.0 μM in cell-free enzymatic assays. Its activity has been confirmed in various in vitro assays. As a proton pump inhibitor, it effectively blocks gastric acid secretion. Its potency is comparable to other PPIs such as omeprazole. The compound is a substituted benzimidazole that is designed for the treatment of gastric ulcers. |
| 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].
Ilaprazole is used in the treatment of dyspepsia and gastroesophageal reflux disease (GERD). It is a proton pump inhibitor that has been evaluated in clinical studies for the treatment of acid-related disorders. It is effective in reducing gastric acid secretion and is used for the management of gastric ulcers, dyspepsia, and GERD. |
| Enzyme Assay |
The primary in vitro assay for Ilaprazole is a H+/K+-ATPase enzyme activity assay using purified gastric proton pump. The enzyme is incubated with ATP and a substrate, and the production of inorganic phosphate is measured in the presence of the compound. The IC50 of 6.0 μM is determined from dose-response curves. This assay directly measures the compound's ability to inhibit the proton pump.
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| Cell Assay |
In vitro cellular experiments for Ilaprazole involve treating gastric parietal cells with the compound and measuring its effects on acid secretion. The inhibition of acid production can be assessed by measuring the accumulation of the weak base [14C]-aminopyrine, which is trapped in acidic compartments. The compound's effects on H+/K+-ATPase activity in intact cells can also be assessed.
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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. In vivo animal experiments for Ilaprazole involve administering the compound to animal models of gastric ulcer or acid hypersecretion. The compound's effects on gastric acid secretion, ulcer formation, and healing are assessed. It is typically administered orally, and its pharmacokinetic parameters, such as absorption and half-life, are determined. |
| ADME/Pharmacokinetics |
Ilaprazole has a molecular weight of 366.44 and a molecular formula of C19H18N4O2S. It is soluble in DMSO (72 mg/mL, 196.48 mM). The compound is a substituted benzimidazole drug candidate. It is typically used as a research reagent and has a purity of 98%. It is stored at -20°C for long-term stability.
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| Toxicity/Toxicokinetics |
Ilaprazole is a research compound that is not intended for human use. Its toxicological profile is characteristic of proton pump inhibitors. Common adverse effects of PPIs include headache, diarrhea, and nausea. Long-term use may be associated with vitamin B12 deficiency and increased risk of bone fractures. Its safety has been evaluated in preclinical and clinical studies for the treatment of acid-related disorders.
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| References |
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| Additional Infomation |
Ilaprazole is a sulfoxide compound belonging to the benzimidazole class. Itprazole has been used to treat Helicobacter pylori infection. Itprazole is a substituted benzimidazole prodrug with selective and irreversible proton pump inhibitory activity. Ilaprazole is a weak base that accumulates in the acidic environment of the secretory tubules of gastric parietal cells, where it is converted to its active sulfinamide form. This sulfinamide form binds to the cysteine sulfhydryl group on the luminal side of the proton pump potassium hydrogen ATPase (H+/K+ ATPase), thereby inhibiting the pump's activity and preventing parietal cells from secreting H+ ions into the gastric lumen, the final step in gastric acid production.
Ilaprazole (IY-81149) is a proton pump inhibitor that inhibits H+/K+-ATPase with an IC50 of 6.0 μM. It is a substituted benzimidazole drug candidate designed for the treatment of gastric ulcers. Ilaprazole is used in the treatment of dyspepsia and gastroesophageal reflux disease (GERD). It is a small molecule with a molecular weight of 366.44. |
| 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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