Rabeprazole(Synonyms: 雷贝拉唑; LY307640)

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Rabeprazole (Synonyms: 雷贝拉唑; LY307640)

Rabeprazole (LY307640) 是一种二代质子泵抑制剂 (pump inhibitor, PPI)，不可逆地抑制胃 H+/K+-ATPase。Rabeprazole 诱导细胞凋亡 (apoptosis)。Rabeprazole 也抑制尿苷核苷核糖水解酶 (UNH) ，IC50 为 0.3 μM。Rabeprazole 可用于胃溃疡和胃食管反流的研究。

Rabeprazole(Synonyms: 雷贝拉唑; LY307640)

Rabeprazole Chemical Structure

CAS No. : 117976-89-3

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Rabeprazole 的其他形式现货产品:

Rabeprazole sodium Rabeprazole Sulfide

生物活性

Rabeprazole (LY307640) is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H+/K+-ATPase. Rabeprazole induces apoptosis. Rabeprazole acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 of 0.3 μM. Rabeprazole can be used for the research of gastric ulcerations and gastroesophageal reflux[1][2][3].

IC50 & Target

Pump inhibitor (PPI)[1]
IC50: 0.3 μM (UNH)[1]
H+/K+-ATPase[2]
Apoptosis[2]
体外研究
(In Vitro)

Rabeprazole attenuates the cell viability of the human gastric cancer cells following treatment with 0.2 mM for 16 hours[2].
Rabeprazole completely inhibits the phosphorylation of ERK1/2 in the MKN-28 cells. The gastric cancer cell line MKN-28 is cultured in acidic culture media (pH 5.4) for 2 hours. Pretreatment with Rabeprazole (0.2 mM for 2 hours) leads to strong inhibition of ERK1/2 phosphorylation in the MKN-28 cells[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: Three gastric cancer cell lines KATO III, MKN-28 and MKN-45
Concentration: 0.2 mM
Incubation Time: 16 hours
Result: Treatment resulted in the attenuation of viability in all cancer cell lines tested, the cell viability of the MKN-28 cells significantly decreased compared with the KATO III and MKN-45 cells, respectively.

Cell Viability Assay[2]

Cell Line: Three gastric cancer cell lines (KATO III, MKN-28 and MKN-45)[2]
Concentration: 0.2 mM
Incubation Time: Pretreatment for 2 hours
Result: Led to strong inhibition of ERK 1/2 phosphorylation in the MKN-28 cells, but a similar effect was not observed in the KATO III and MKN-45 cells.

体内研究
(In Vivo)

Rabeprazole (10 mg/kg; P.O.; every 48 h for 18 weeks) course leads to a significant decline in bone mineral density (BMD) and decreases serum calcium level and produces secondary hyperparathyroidism in female mice[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female Swiss albino mice (body weight equals 18-26 g)[3]
Dosage: 10 mg/kg
Administration: Oral administration; every 48 h for 18 weeks
Result: Showed significantly lower serum calcium level compared to the vehicle treated group (5.5±2.07 vs. 9.68±2.77).

Clinical Trial

分子量

359.44

Formula

C18H21N3O3S
CAS 号

117976-89-3
中文名称

雷贝拉唑
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
溶解性数据
In Vivo:
  • 1.

    Rabeprazole was dissolved in distilled water[3].
参考文献

  • [1]. Tara A Shea, et al. Identification of Proton-Pump Inhibitor Drugs That Inhibit Trichomonas Vaginalis Uridine Nucleoside Ribohydrolase. Bioorg Med Chem Lett. 2014 Feb 15;24(4):1080-4.

    [2]. Mengli Gu, et al. Rabeprazole Exhibits Antiproliferative Effects on Human Gastric Cancer Cell Lines. Oncol Lett. 2014 Oct;8(4):1739-1744.

    [3]. Aly A M Shaalan, et al. Supplement With Calcium or Alendronate Suppresses Osteopenia Due to Long Term Rabeprazole Treatment in Female Mice: Influence on Bone TRAP and Osteopontin Levels. Front Pharmacol. 2020 May 13;11:583.

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