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Rabeprazole/雷贝拉唑 {[allProObj[0].p_purity_real_show]}

货号:A229737 同义名: LY307640

Rabeprazole 是一种抗溃疡化合物,能够不可逆地抑制胃 H+/K+ ATP 酶泵,IC50 为 72 nM。

Rabeprazole/雷贝拉唑 化学结构 CAS号:117976-89-3
Rabeprazole/雷贝拉唑 化学结构
CAS号:117976-89-3
Rabeprazole/雷贝拉唑 3D分子结构
CAS号:117976-89-3
Rabeprazole/雷贝拉唑 化学结构 CAS号:117976-89-3
Rabeprazole/雷贝拉唑 3D分子结构 CAS号:117976-89-3
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Rabeprazole/雷贝拉唑 纯度/质量文件 产品仅供科研

货号:A229737 标准纯度: {[allProObj[0].p_purity_real_show]}
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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。

Rabeprazole/雷贝拉唑 生物活性

靶点
  • Proton Pump

描述 Rabeprazole is an antiulcer drug and selective and irreversible inhibitor of the gastric H+/K+ ATPase pump (IC50 = 72 nM).

Rabeprazole/雷贝拉唑 细胞实验

Cell Line
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.

Rabeprazole/雷贝拉唑 动物实验

Species
Animal Model
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

Rabeprazole/雷贝拉唑 临床研究

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 <<

Rabeprazole/雷贝拉唑 参考文献

[1]Yamasaki Y, Fujimura T, et al. Effects of rabeprazole on bone metabolic disorders in a gastrectomized rat model. Biomed Rep. 2016 Jul;5(1):118-124.

[2]Iwakiri R, Tominaga K, et al. Randomised clinical trial: rabeprazole improves symptoms in patients with functional dyspepsia in Japan. Aliment Pharmacol Ther. 2013 Oct;38(7):729-40.

Rabeprazole/雷贝拉唑 实验方案

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

Rabeprazole/雷贝拉唑 技术信息

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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