Ilaprazole

製品コードS3666 バッチS366601

印刷

化学情報

Chemical Structure Synonyms IY-81149 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C19H18N4O2S
分子量 366.44 CAS No. 172152-36-2
Solubility (25°C)* 体外 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.

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生物活性

製品説明 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.
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].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 human colon cancer HCT 116, ES-2, A549 and SW1990 cells
濃度 0-100 μM
反応時間 24 or 48 h
実験の流れ

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).
動物実験 動物モデル Male Sprague-Dawely (SD) rats
投薬量 3, 10, 30 mg/kg
投与方法 Intraduodenally and orally

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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