Ilaprazole

For research use only.

Catalog No.S3666 Synonyms: IY-81149

1 publication

Ilaprazole Chemical Structure

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.

Selleck's Ilaprazole has been cited by 1 publication

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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

Cell Research:

[1]

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  • 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).


    (Only for Reference)
Animal Research:

[2]

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

Solubility (25°C)

In vitro DMSO 73 mg/mL (199.21 mM)
Water Insoluble
Ethanol '14 mg/mL

* 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.

Chemical Information

Molecular Weight 366.44
Formula

C19H18N4O2S

CAS No. 172152-36-2
Storage powder
in solvent
Synonyms IY-81149
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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID