Home Transmembrane Transporters Proton Pump inhibitor - ATPase inhibitor Ilaprazole

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Ilaprazole Proton Pump inhibitor

Cat.No.S3666

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 Proton Pump inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 366.44

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Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 366.44 Formula

C19H18N4O2S

 Storage (From the date of receipt)
CAS No. 172152-36-2 Download SDF Storage of Stock Solutions

Synonyms IY-81149 Smiles CC1=C(C=CN=C1CS(=O)C2=NC3=C(N2)C=C(C=C3)N4C=CC=C4)OC

Solubility

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

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 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
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Mechanism of Action

Targets/IC50/Ki
Proton pump [2]
H+/K+-ATPase [2]
(Cell-free assay)
6 μM
TOPK [1]
111 μM(Kd)
In vitro
Ilaprazole inhibited TOPK activities with high affinity and selectivity[1]. In vitro studies showed that this compound inhibited TOPK activities in HCT116, ES-2, A549, SW1990 cancer cells. It was also found to induce the cleavage of poly-(ADP-ribose) polymerase (PARP), a DNA repair regulatory protein. In rabbit parietal cell preparation, this chemical 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 this compound-treated tumor tissues. The toxicological data showed that the LD50 of this chemical was more than 5000 mg/kg in rats[1]. In pylorus-ligated rats, this compound had a strong and long-lasting antisecretory activity despite of its instability in acidic solution. It strongly inhibited secretagogues stimulated gastric acid secretion in rats and dogs[2].
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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 --

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