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| 产品名称 | Proton Pump ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Zinc pyrithione | ✔ | 98+% | |||||||||||||||||
| PF 03716556 |
++++
H+/K+-ATPase, pIC50: ~6.5 |
99% | |||||||||||||||||
| Lansoprazole | ✔ | 98% | |||||||||||||||||
| Esomeprazole Magnesium | ✔ | 98%+ | |||||||||||||||||
| Rabeprazole | ✔ | 99%+ | |||||||||||||||||
| Ilaprazole | ✔ | TOPK | 97% | ||||||||||||||||
| Bafilomycin A1 |
++++
H+-ATPase, IC50: 0.44 nM |
99% | |||||||||||||||||
| Pantoprazole sodium | ✔ | 98% | |||||||||||||||||
| (R)-Lansoprazole | ✔ | 98% | |||||||||||||||||
| Tenatoprazole | ✔ | 99%+ | |||||||||||||||||
| Omeprazole | ✔ | 98% | |||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 靶点 |
|
| 描述 | Rabeprazole is an antiulcer drug and selective and irreversible inhibitor of the gastric H+/K+ ATPase pump (IC50 = 72 nM). |
| Concentration | Treated Time | Description | References | |
| Dematiaceous fungi | 2-128 mg/ml | 72h | Rabeprazole alone exhibited limited antifungal effect against all tested species. However, the median MICs of azoles and RAB in the combination revealed up to 7.7-fold and 128-fold reduction compared to that when tested alone, respectively. | Front Cell Infect Microbiol. 2024 Jan 17;14:1296151. |
| Candida spp. | 2-128 mg/ml | 24h | Rabeprazole alone exhibited limited antifungal effect against all tested species. However, the median MICs of azoles and RAB in the combination revealed up to 7.7-fold and 128-fold reduction compared to that when tested alone, respectively. | Front Cell Infect Microbiol. 2024 Jan 17;14:1296151. |
| Aspergillus fumigatus | 2-128 mg/ml | 48h | Rabeprazole alone exhibited limited antifungal effect against all tested species. However, the median MICs of azoles and RAB in the combination revealed up to 7.7-fold and 128-fold reduction compared to that when tested alone, respectively. | Front Cell Infect Microbiol. 2024 Jan 17;14:1296151. |
| Trypanosoma cruzi epimastigotes | 250 μM | 24 hours | To evaluate the effect of Rabeprazole on cell viability and TIM enzyme activity with different numbers of parasites. Results showed that Rabeprazole significantly reduced cell viability and TIM enzyme activity. | J Enzyme Inhib Med Chem. 2023 Dec;38(1):2231169. |
| Trypanosoma cruzi epimastigotes | 100–2000 μM | 4 hours | To evaluate the effect of Rabeprazole on cell viability and TIM enzyme activity. Results showed that Rabeprazole significantly reduced cell viability and TIM enzyme activity. | J Enzyme Inhib Med Chem. 2023 Dec;38(1):2231169. |
| Campylobacter jejuni and C. coli | 16 µg/ml | Immediately | RPZ-TH and PPIs also inhibited the motility of C. jejuni and C. coli, but had no effect on other bacteria such as V. cholerae and S. enterica. | Antimicrob Agents Chemother. 2000 Nov;44(11):3069-73. |
| Helicobacter pylori | 16 µg/ml | Immediately | Rabeprazole (RPZ) and its thioether derivative (RPZ-TH) markedly inhibited the motility of H. pylori. RPZ-TH completely blocked motility at 1 µg/ml, while RPZ had an IC50 of 16 µg/ml. | Antimicrob Agents Chemother. 2000 Nov;44(11):3069-73. |
| Human lung microvascular endothelial cells (HLMVECs) | 20 μM | 18 hours | Rabeprazole induced HIF1A mRNA expression in a dose-dependent manner | Cells. 2022 Apr 22;11(9):1425. |
| Trypanosoma cruzi epimastigotes | 1 mM | 4 hours | To evaluate the effect of Rabeprazole on cell viability and TIM enzyme activity with different numbers of parasites in a short time. Results showed that Rabeprazole significantly reduced cell viability and TIM enzyme activity. | J Enzyme Inhib Med Chem. 2023 Dec;38(1):2231169. |
| Human lung microvascular endothelial cells (HLMVECs) | 20 μM | 18 hours | Rabeprazole induced HIF1A mRNA expression in a dose-dependent manner | Cells. 2022 Apr 22;11(9):1425. |
| HEK293 cells | 100 μM | 48 hours | Rabeprazole significantly reduced the transcriptional activity of the CDX2 promoter. | Front Pharmacol. 2024 Nov 7;15:1409001. |
| AGS cells | 100 μM | 48 hours | Rabeprazole significantly downregulated CDX2 and MUC2 mRNA and protein levels, alleviating gastric intestinal metaplasia. | Front Pharmacol. 2024 Nov 7;15:1409001. |
| BGC823 cells | 100 μM | 48 hours | Rabeprazole inhibited CREB phosphorylation and nuclear translocation, reducing the binding of CREB to the GPX4 promoter, thereby decreasing GPX4 expression and inducing ferroptosis. | Front Pharmacol. 2024 Nov 7;15:1409001. |
| Administration | Dosage | Frequency | Description | References | ||
| B10.RIII mice | Experimental autoimmune uveitis (EAU) model | Intraperitoneal injection | 60 mg/kg/day | Once daily for 7 days (from Day 7 to Day 14) | To evaluate the effect of rabeprazole on the EAU mouse model. Results showed that rabeprazole reduced anterior chamber inflammation and retinal inflammation, inhibited TNF and IL-1β expression, and promoted IL-10 expression. | Front Immunol. 2022 Jun 21;13:895869 |
| C57BL/6 mice | DNBS and DSS-induced colitis models | Oral | 30 mg/kg | Twice daily, throughout the experiment | Rabeprazole failed to demonstrate any anti-colitic effect | Front Immunol. 2022 May 25;13:870817 |
| Mice | Endotoxemia-induced inflammatory lung injury model | Oral | 18 mg/kg | Administered at 4 and 20 hours post-LPS | Rabeprazole promotes vascular repair and resolution of inflammatory lung injury through HIF-1α/FoxM1 signaling | Cells. 2022 Apr 22;11(9):1425. |
| Wistar rats | Anesthetized rat model | Intravenous injection | 4 mg/kg | Single dose, lasting 2 hours | To investigate the effects of Rabeprazole on the concentration of amoxicillin in gastric juice and gastric mucosa. Results showed that Rabeprazole increased the amoxicillin concentration in gastric juice but did not significantly alter its concentration in blood or gastric mucosa. | Acta Pharmacol Sin. 2010 Apr;31(4):501-8 |
| Female Swiss albino mice | Osteoporosis model | Oral | 10 mg/kg every 48 hours | Every 48 hours for 18 weeks | To investigate the impact of rabeprazole on osteoporosis and explore the modulatory effects of dietary calcium or alendronate on this side effect. Results showed that rabeprazole significantly reduced bone mineral density, increased trabecular separation and osteoclast number. Calcium supplementation or alendronate partially restored bone density and reduced osteoclast activity. | Front Pharmacol. 2020 May 13;11:583 |
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT01408186 | Upper Gastrointestinal Bleedin... 展开 >>g 收起 << | Phase 3 | Completed | - | Hong Kong ... 展开 >> Prince of Wales Hospital Hong Kong, Hong Kong Japan Second Department of Internal Medicine, Shimane University Faculty of Medicine, Izumo, Japan Izumo, Japan Department of Molecular Gastroenterology and Hepatology, Kyoto Prefectural University of Medicine, Kyoto, Japan Kyoto, Japan Department of Gastroenterology, Osaka City General Hospital, Osaka, Japan (Satellite hospital of Osaka City University) Osaka, Japan Department of Gastroenterology, Osaka City University Graduate School of Medicine Osaka, Japan Department of Gastroenterology, Takarazuka Municipal Hospital, Hyogo, Japan (Satellite hospital of Osaka City University) Osaka, Japan Second Department of Internal Medicine, Osaka Medical College, Takatsuki, Osaka, Japan Osaka, Japan Department of Internal Medicine and Gastroenterology, Saga Medical School, Saga, Japan Saga, Japan 收起 << |
| NCT03658733 | Helicobacter Pylori Infection | Phase 4 | Not yet recruiting | October 31, 2019 | China, Shandong ... 展开 >> Xiuli Zuo Recruiting Jinan, Shandong, China Contact: Xiuli Zuo, PhD,MD 15588818685 ext 053188369277 zuoxiuli@sina.com Sub-Investigator: Yue Li, MD Sub-Investigator: Chaoran Ji, MD 收起 << |
| NCT01918176 | Healthy | Phase 1 | Completed | - | United States, Florida ... 展开 >> Pfizer Investigational Site South Miami, Florida, United States, 33143 收起 << |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.78mL 0.56mL 0.28mL |
13.91mL 2.78mL 1.39mL |
27.82mL 5.56mL 2.78mL |
|
| CAS号 | 117976-89-3 |
| 分子式 | C18H21N3O3S |
| 分子量 | 359.44 |
| SMILES Code | COCCCOC1=C(C)C(CS(=O)C2=NC3=C(N2)C=CC=C3)=NC=C1 |
| MDL No. | MFCD00868879 |
| 别名 | LY307640 |
| 运输 | 蓝冰 |
| InChI Key | YREYEVIYCVEVJK-UHFFFAOYSA-N |
| Pubchem ID | 5029 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry, 2-8°C |
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