Home Transmembrane Transporters Proton Pump inhibitor - ATPase inhibitor Ilaprazole For research use only.

Ilaprazole

Synonyms: IY-81149

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

Ilaprazole Chemical Structure

CAS: 172152-36-2

Selleck's Ilaprazole has been cited by 1 publication

Purity & Quality Control

Batch: S366601 DMSO] 73 mg/mL] false] Ethanol] 14 mg/mL] false] Water] Insoluble] false Purity: 99.50%
99.50

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Signaling Pathway

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Proton Pump Signaling Pathway

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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
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].
Cell Research 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).
In Vivo
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].
Animal Research Animal Models Male Sprague-Dawely (SD) rats
Dosages 3, 10, 30 mg/kg
Administration Intraduodenally and orally
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05617651 Not yet recruiting
Pharmacokinetics
Il-Yang Pharm. Co. Ltd.
 November 30 2024 Phase 1
NCT05558150 Completed
Drug Interaction Potentiation
Il-Yang Pharm. Co. Ltd.
 November 10 2022 Phase 1
NCT05509543 Recruiting
Pharmacokinetics
Il-Yang Pharm. Co. Ltd.
 August 24 2022 Phase 1
NCT03099876 Unknown status
Helicobacter Pylori Infection
Il-Yang Pharm. Co. Ltd.
 March 1 2017 --

Chemical Information & Solubility

Molecular Weight 366.44 Formula

C19H18N4O2S
CAS No. 172152-36-2 SDF Download Ilaprazole SDF
Smiles CC1=C(C=CN=C1CS(=O)C2=NC3=C(N2)C=C(C=C3)N4C=CC=C4)OC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 73 mg/mL ( (199.21 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 14 mg/mL

Water : Insoluble


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In vivo
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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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