Ilaprazole

Catalog No.S3666 Batch:S366601

Technical Data

Formula	C₁₉H₁₈N₄O₂S
Molecular Weight	366.44	CAS No.	172152-36-2
Solubility (25°C)*	In vitro	DMSO	73 mg/mL (199.21 mM)
		Ethanol	14 mg/mL (38.2 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 Assay:^{^[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 Study:^{^[2]}	Animal Models Male Sprague-Dawely (SD) rats Dosages 3, 10, 30 mg/kg Administration Intraduodenally and orally

Cell Assay:^{^[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 Study:^{^[2]}

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

References

Selleck's Ilaprazole has been cited by 2 publications

A drug repurposing study identifies novel FOXM1 inhibitors with in vitro activity against breast cancer cells [ Med Oncol, 2024, 41(8):188]	PubMed: 38918225
Ilaprazole and other novel prazole-based compounds that bind Tsg101 inhibit viral budding of HSV-1/2 and HIV from cells [ J Virol, 2021, JVI.00190-21]	PubMed: 33731460

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SHIPPING AND STORAGE
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