Rabeprazole sodium(Synonyms: 雷贝拉唑钠; LY307640 sodium)

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Rabeprazole sodium (Synonyms: 雷贝拉唑钠; LY307640 sodium) 纯度: 99.17%

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。

Rabeprazole sodium(Synonyms: 雷贝拉唑钠; LY307640 sodium)

Rabeprazole sodium Chemical Structure

CAS No. : 117976-90-6

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10 mM * 1 mL in DMSO ￥550 In-stock
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50 mg ￥921 In-stock
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生物活性

Rabeprazole sodium (LY307640 sodium) is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H+/K+-ATPase. Rabeprazole sodium induces apoptosis. Rabeprazole sodium acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 of 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].

上海金畔生物科技有限公司 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.

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.

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].

上海金畔生物科技有限公司 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

381.42

Formula

C18H20N3NaO3S
CAS 号

117976-90-6
中文名称

雷贝拉唑钠
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
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 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。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 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 上海金畔生物科技有限公司 网站选购。
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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