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Rebamipide (OPC12759) 是一種口服有效的胃保護(hù)劑。Rebamipide 通過誘導(dǎo) COX-2 的表達(dá)來增強(qiáng)內(nèi)源性 PGs 的產(chǎn)生 (特別是胃內(nèi) PGE2),從而保護(hù)胃粘膜免受傷害。Rebamipide 還具有抗胃癌細(xì)胞增殖活性。Rebamipide 可用于粘膜保護(hù)、胃十二指腸潰瘍,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 endogenous PGs (especially intragastric PGE2) by inducing COX-2 expression, thereby protecting the gastric mucosa from injury. Rebamipide exerts anti-proliferative activity against gastric cancer cells. Rebamipide can be used in studies of mucosal protection, gastroduodenal ulcer, gastritis and gastric cancer[1][2].
IC50 & Target[1]
COX-2 PGE2
體外研究(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. |
體內(nèi)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 PGE2 in a dose-dependent manner. (PGE2 is 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. |
分子量:370.79
Formula:C19H15ClN2O4
CAS 號:90098-04-7
中文名稱:瑞巴派特
運(yùn)輸條件:Room temperature in continental US; may vary elsewhere.
儲存方式
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
溶解性數(shù)據(jù)
DMSO : 50 mg/mL (134.85 mM; Need ultrasonic)
H2O : 0.1 mg/mL (0.27 mM; Need ultrasonic)
濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
---|
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 |
請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 儲存時,請在 6 個月內(nèi)使用,-20°C 儲存時,請在 1 個月內(nèi)使用。
以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用; 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶
參考文獻(xiàn)
Rebamipide (OPC12759) 是一種口服有效的胃保護(hù)劑。Rebamipide 通過誘導(dǎo) COX-2 的表達(dá)來增強(qiáng)內(nèi)源性 PGs 的產(chǎn)生 (特別是胃內(nèi) PGE2),從而保護(hù)胃粘膜免受傷害。Rebamipide 還具有抗胃癌細(xì)胞增殖活性。Rebamipide 可用于粘膜保護(hù)、胃十二指腸潰瘍,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 endogenous PGs (especially intragastric PGE2) by inducing COX-2 expression, thereby protecting the gastric mucosa from injury. Rebamipide exerts anti-proliferative activity against gastric cancer cells. Rebamipide can be used in studies of mucosal protection, gastroduodenal ulcer, gastritis and gastric cancer[1][2].
IC50 & Target[1]
COX-2 PGE2
體外研究(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. |
體內(nèi)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 PGE2 in a dose-dependent manner. (PGE2 is 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. |
分子量:370.79
Formula:C19H15ClN2O4
CAS 號:90098-04-7
中文名稱:瑞巴派特
運(yùn)輸條件:Room temperature in continental US; may vary elsewhere.
儲存方式
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
溶解性數(shù)據(jù)
DMSO : 50 mg/mL (134.85 mM; Need ultrasonic)
H2O : 0.1 mg/mL (0.27 mM; Need ultrasonic)
濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
---|
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 |
請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 儲存時,請在 6 個月內(nèi)使用,-20°C 儲存時,請在 1 個月內(nèi)使用。
以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用; 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶
參考文獻(xiàn)