Rabeprazole sodium (LY307640 sodium) 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 sodium 诱导细胞凋亡 (apoptosis)。Rabeprazole sodium 也抑制尿苷核苷核糖水解酶 (UNH) ，IC50为 0.3 μM。Rabeprazole sodium 可用于胃溃疡和胃食管反流的研究。
| 生物活性 | Rabeprazole sodium (LY307640 sodium) is a second-generation protonpump inhibitor(PPI) that irreversibly inactivates gastric H+/K+-ATPase. Rabeprazole sodium inducesapoptosis. Rabeprazole sodium acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with anIC50of 0.3 μM. Rabeprazole sodium 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 ERK 1/2 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. |
Western Blot Analysis[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 | 4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
| 溶解性数据 | In Vitro: H2O : ≥ 100 mg/mL(262.18 mM) DMSO : ≥ 48 mg/mL(125.85 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 2.6218 mL | 13.1089 mL | 26.2178 mL | | 5 mM | 0.5244 mL | 2.6218 mL | 5.2436 mL | | 10 mM | 0.2622 mL | 1.3109 mL | 2.6218 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (stored under nitrogen)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (5.45 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.45 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (5.45 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.45 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (5.45 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.45 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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