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。
| 生物活性 | Rabeprazole (LY307640) is a second-generation protonpump inhibitor(PPI) that irreversibly inactivates gastric H+/K+-ATPase. Rabeprazole inducesapoptosis. Rabeprazole acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with anIC50of 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].
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. |
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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].
| 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). |
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| 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].
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