Pantoprazole sodium 是一种具有口服活性的质子泵抑制剂,是一种取代的苯并咪唑,是H+/K+-ATPase抑制剂,IC50为 6.8 μM。它可以改善 pH 值稳定性,具有抗分泌和抗溃疡的作用。它联合阿霉素可显著增加肿瘤生长延迟。
产品描述
Pantoprazole Sodium is the sodium salt form of a substituted benzimidazole with proton pump inhibitor activity. Pantoprazole is a lipophilic, weak base that crosses the parietal cell membrane and enters the acidic parietal cell canaliculus where it becomes protonated, producing the active metabolite sulfenamide, which forms an irreversible covalent bond with two sites of the H+/K+-ATPase enzyme located on the gastric parietal cell, thereby inhibiting both basal and stimulated gastric acid production.
体外活性
pantoprazole (PPZ) inhibits tumor cells proliferation, inducs apoptosis and decreases the expression of HIF-1α protein[2]. Pantoprazole affects the intracellular distribution of HIF-1α in SGC-7901 cells, which might be one of the mechanisms of its chemosensitizing effect on cancer cells[3].
体内活性
After PPZ treatment, apoptotic cell death is seen selectively in cancer cells and is accompanied with extracellular signal-regulated kinase deactivation. By contrast, normal gastric mucosal cells show the resistance to PPZ-induced apoptosis through the overexpression of antiapoptotic regulators including HSP70 and HSP27. In a xenograft model of nude mice, administration of PPZ significantly inhibits tumorigenesis and induces large-scale apoptosis of tumor cells[4].
细胞实验
Pantoprazole sodium salts are resuspended in normal saline (0.85%) at 5 mg/ml immediately prior to use. When the SGC-7901 cells have reached 60–70% confluence, PPZ is added at a final concentration of 20 µg/ml, and the cells are cultured for additional experiments. For example, The SGC-7901 cells are seeded in 100 µl of medium per well, at a density of 1×104/well, in 96-well plates and treated with PPZ for 24 h. (Only for Reference)
Cas No.
138786-67-1
分子式
C16H14F2N3NaO4S
分子量
405.35
别名
BY-1023 sodium;泮托拉唑钠;泮托拉唑钠盐;SKF96022 sodium;Pantecta;BY1023 (sodium);Pantoloc;SKF96022 (sodium)
储存和溶解度
DMSO:75 mg/mL (185 mM)
H2O:74 mg/mL (182.6 mM)
Ethanol:75 mg/mL (185 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years