For research use only.
Catalog No.S3666 Synonyms: IY-81149
CAS No. 172152-36-2
Ilaprazole (IY-81149) is a new proton pump inhibitor (PPI) used in the treatment of dyspepsia, peptic ulcer disease (PUD), gastroesophageal reflux disease (GORD/GERD) and duodenal ulcer. It inhibits H+/K+-ATPase with an IC50 of 6.0 μM.
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Choose Selective Proton Pump Inhibitors
|Description||Ilaprazole (IY-81149) is a new proton pump inhibitor (PPI) used in the treatment of dyspepsia, peptic ulcer disease (PUD), gastroesophageal reflux disease (GORD/GERD) and duodenal ulcer. It inhibits H+/K+-ATPase with an IC50 of 6.0 μM.|
Ilaprazole inhibited TOPK activities with high affinity and selectivity. In vitro studies showed that ilaprazole inhibited TOPK activities in HCT116, ES-2, A549, SW1990 cancer cells. Ilaprazole was also found to induce the cleavage of poly-(ADP-ribose) polymerase (PARP), a DNA repair regulatory protein. In rabbit parietal cell preparation, IY-81149 irreversibly inhibited H+/K+-ATPase in dose-dependent manner with an IC50 of pump inhibitory activity of 6.0×10-6 mol/l.
|In vivo||Ilaprazole could suppress tumor growth by inhibiting TOPK activities in vivo. The phosphorylations of histone H3 (Ser10) were significantly inhibited in ilaprazole-treated tumor tissues. The toxicological data showed that the LD50 of ilaprazole was more than 5000 mg/kg in rats. In pylorus-ligated rats, IY-81149 had a strong and long-lasting antisecretory activity despite of its instability in acidic solution. IY-81149 strongly inhibited secretagogues stimulated gastric acid secretion in rats and dogs.|
|In vitro||DMSO||73 mg/mL (199.21 mM)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).
Molecular Weight Calculator
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03099876||Unknown status||Procedure: treatment period||Helicobacter Pylori Infection||Il-Yang Pharm. Co. Ltd.||March 1 2017||--|
|NCT01688544||Completed||Drug: Ilaprazole||Healthy||Inje University||January 2009||Phase 1|
|NCT01820143||Completed||Drug: Ilaprazole|Drug: Esomeprazole||Healthy|Pharmacokinetics|Pharmacodynamics|Ilaprazole||Il-Yang Pharm. Co. Ltd.||February 2005||Phase 1|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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