Rebamipide (OPC12759) 是一种口服有效的胃保护剂。Rebamipide 通过诱导COX-2的表达来增强内源性PGs的产生 (特别是胃内PGE2)，从而保护胃粘膜免受伤害。Rebamipide 还具有抗胃癌细胞增殖活性。Rebamipide 可用于粘膜保护、胃十二指肠溃疡，胃炎和胃癌的研究。
| 生物活性 | Rebamipide (OPC12759) is an orally active gastroprotective agent that enhances the production of endogenousPGs(especially intragastricPGE2) by inducingCOX-2expression, thereby protecting the gastric mucosa from injury. Rebamipide exerts anti-proliferative activity against gastriccancercells. Rebamipide can be used in studies of mucosal protection, gastroduodenal ulcer, gastritis and gastriccancer[1][2]. |
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体外研究
(In Vitro) | Rebamipide (1.4, 2.7, 5.4 mM; 24 h) inhibits proliferation of gastric cancer cell[1].
Rebamipide (5.4 mM; 30 min) activates Smad signaling pathway in AGS cells[1].
Rebamipide (5.4 mM; 3 h) induces the expression of Cdk inhibitor p21 in AGS cells[1].
Cell Proliferation Assay[1] | Cell Line: | AGS cells | | Concentration: | 1.4, 2.7, 5.4 mM | | Incubation Time: | 24 h | | Result: | Significant decreased in cell proliferation in a concentration-dependent manner. |
Western Blot Analysis[1] | Cell Line: | AGS cells | | Concentration: | 5.4 mM | | Incubation Time: | 30 min or 3 h | | Result: | Significantly increased phosphorylation of Smad2/3 by 1.2-fold when at 30 min and formation of Smad2/3-Smad4 complex by 1.4-fold.
Upregulated expression of p21 protein by 2.5-fold when at 3 h. |
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体内研究
(In Vivo) | Rebamipide (5, 15, 50 mg/kg; p.o.; once daily for 14 days) enhances the expression of COX-2 and PGE2, and protects gastric mucosa from acid-induced injury in rat gastric mucosa[2].
| Animal Model: | Specific pathogen-free male Sprague-Dawley rats (200-230 g; 7-week-old)[2]. | | Dosage: | 5, 15, 50 mg/kg | | Administration: | Oral administration; once daily for 14 days. | | Result: | Increased the level of COX-2 immunoreactivity and PGE2in a dose-dependent manner. (PGE2is implicated in protection of gastric mucosa from various insults and acceleration of gastric wound healing).
Inhibited intragastric HCl administration-induced gastric mucosal bleeding and erosion. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 33.33 mg/mL(89.89 mM;Need ultrasonic) H2O : 0.1 mg/mL(0.27 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.6969 mL | 13.4847 mL | 26.9694 mL | | 5 mM | 0.5394 mL | 2.6969 mL | 5.3939 mL | | 10 mM | 0.2697 mL | 1.3485 mL | 2.6969 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。-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: 2.5 mg/mL (6.74 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (6.74 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 25.0 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%corn oil Solubility: ≥ 2.5 mg/mL (6.74 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.74 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 25.0 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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