Ilaprazole

製品コードS3666 バッチS366601

印刷

化学情報

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

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Ilaprazole (IY-81149) は、消化不良、消化性潰瘍 (PUD)、胃食道逆流症 (GORD/GERD)、および十二指腸潰瘍の治療に使用される新しいプロトンポンプ阻害薬 (PPI) です。これは 6.0 μM の IC50 で H+/K+-ATPase を阻害します。
in vitro	Ilaprazole inhibited TOPK activities with high affinity and selectivity. 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.
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. 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.

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 this compound 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 this compound 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

参考

https://pubmed.ncbi.nlm.nih.gov/28388576/
https://pubmed.ncbi.nlm.nih.gov/11304936/

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：

Evasion of CARD8 Activation During HIV-1 Assembly [ bioRxiv, 2025, 2025.05.19.654850]	PubMed: 40475532
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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。