Ilaprazole

Catalog No.S3666 Synonyms: IY-81149

For research use only.

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 Chemical Structure

CAS No. 172152-36-2

Selleck's Ilaprazole has been cited by 1 Publication

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Biological Activity

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.
Targets
Proton pump [2] H+/K+-ATPase [2]
(Cell-free assay)
TOPK [1]
6 μM 111 μM(Kd)
In vitro

Ilaprazole inhibited TOPK activities with high affinity and selectivity[1]. 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[2].

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[1]. 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[2].

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: human colon cancer HCT 116, ES-2, A549 and SW1990 cells
  • Concentrations: 0-100 μM
  • Incubation Time: 24 or 48 h
  • Method:

    To estimate cell viability, human colon cancer HCT 116, ES-2, A549 and SW1990 cells (5000 cells/well) were seeded in 96-well plates for 24 h at 37°C in a 5% CO2 incubator. The attached cells were fed with fresh medium containing various concentrations of ilaprazole (0-100 μM) for additional 24 h and 48 h. After culturing for various times, the cytotoxicity of ilaprazole was measured using a cck8 assay kit. All experiments were performed in triplicate, and the mean absorbance values were calculated. The results are expressed as the percentage of inhibition that produced a reduction in absorbance by ilaprazole treatment compared with the non-treated cells (control).

Animal Research:

[2]

  • Animal Models: Male Sprague-Dawely (SD) rats
  • Dosages: 3, 10, 30 mg/kg
  • Administration: Intraduodenally and orally

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 366.44
Formula

C19H18N4O2S

CAS No. 172152-36-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(C=CN=C1CS(=O)C2=NC3=C(N2)C=C(C=C3)N4C=CC=C4)OC

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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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

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.

Handling Instructions

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