艾美拉唑钾盐
中文名称:
艾美拉唑钾盐
中文同义词:
埃索美拉唑钾;埃索拉唑钾盐;6-甲氧基-2-[(S)-[(4-甲氧基-3,5-二甲基-2-吡啶基)甲基]亚磺酰基]-1H-苯并咪唑钾盐;6-甲氧基-2-[(S)-[(4-甲氧基-3,5-二甲基-2-吡啶基)甲基]亚磺酰基]-1H-苯并咪唑钾盐 (1:1);艾美拉唑钾盐;埃索美拉唑钾盐
英文名称:
Esomeprazole potassium
英文同义词:
(S)-Omeprazole potassium;6-Methoxy-2-[(S)-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole potassium salt (1:1);(R)-5-METHOXY-2-((4-METHOXY-3,5-DIMETHYLPYRIDIN-2-YL)METHYLSULFINYL)BENZO[D]IMIDAZOL-1-IDE POTASSIUM SALT;Esomeprazole potassium;(S)-5-methoxy-2-((4-methoxy-3,5-dimethylpyridin-2-yl)methylsulfinyl)-1H-benzo[d];potassium,5-methoxy-2-[(S)-(4-methoxy-3,5-dimethylpyridin-2-yl)methylsulfinyl]benzimidazol-1-ide;1H-Benzimidazole,6-methoxy-2-[(S)-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-,potassium salt (1:1);Esomeprazole potassium USP/EP/BP
CAS号:
161796-84-5
分子式:
C17H19KN3O3S
分子量:
384.51
EINECS号:
相关类别:
医用原料;医药原料药;原料药
Mol文件:
161796-84-5.mol
概述
艾美拉唑钾盐是一种质子泵抑制剂，艾美拉唑钾盐是奥美拉唑的S-异构体，通过特异性的质子泵抑制作用减少胃酸分泌，奥美拉唑的R-异构体和S-异构体具有相似的药效学特性。艾美拉唑钾盐为弱碱性药物，在壁细胞泌酸微管的高酸环境中浓集并转化为活性形式，从而抑制该部位的H+/K+-ATP酶(质子泵)，对基础胃酸分泌和受刺激后的胃酸分泌均产生抑制。
应用
艾美拉唑钾盐盐是通过艾美拉唑钾盐成盐得到的，艾美拉唑钾盐盐能够降低对机体的刺激性，并且在机体中具有良好的溶解性，提高生物利用度，从而能够产生更理想的药理作用，常见的艾美拉唑钾盐盐主要有艾美拉唑钾盐钠盐、艾美拉唑钾盐钾盐、艾美拉唑钾盐镁盐。目前，艾美拉唑钾盐盐主要通过艾美拉唑钾盐成盐得到，因此，艾美拉唑钾盐的制备方法不仅影响艾美拉唑钾盐的纯度，而且影响艾美拉唑钾盐盐的纯度。
生物活性
Esomeprazole potassium salt ((S)-Omeprazole potassium salt) 是一种有效的具有口服活性质子泵抑制剂，可通过抑制胃壁细胞中的 H+, K+-ATPase 来降低酸分泌，并可用于胃食管反流疾病的研究。
靶点
H + , K + -ATPase
体外研究
Esomeprazole (25-100 µM; 20 hours; MDA-MB-468 cells) treatment suppresses growth of triple-negative breast cancer cell in vitro in a dose-dependent manner through increase in their intracellular acidification.
Cell Viability Assay
Cell Line: MDA-MB-468 cells
Concentration: 25 µM, 50 µM, 75 µM, 100 µM
Incubation Time: 20 hours
Result: Suppressed growth of triple-negative breast cancer cell in vitro in a dose-dependent manner.
Cell Line:
MDA-MB-468 cells
Concentration:
25 µM, 50 µM, 75 µM, 100 µM
Incubation Time:
20 hours
Result:
Suppressed growth of triple-negative breast cancer cell in vitro in a dose-dependent manner.
体内研究
Esomeprazole (30-300 mg/kg; oral gavage; daily; for 19 or 11 days; C57BL/6J mice) treatment significantly inhibits the progression of fibrosis throughout the lungs of the animals. Esomeprazole also reduces circulating markers of inflammation and fibrosis.
Animal Model: C57BL/6J mice (8-weeks old, 25-30 g) treated with cotton smoke-induced lung injury
Dosage: 30 mg/kg, 300 mg/kg
Administration: Oral gavage; daily; for 19 or 11 days
Result: Significantly inhibited the progression of fibrosis throughout the lungs of the animals.
Animal Model:
C57BL/6J mice (8-weeks old, 25-30 g) treated with cotton smoke-induced lung injury
Dosage:
30 mg/kg, 300 mg/kg
Administration:
Oral gavage; daily; for 19 or 11 days
Result:
Significantly inhibited the progression of fibrosis throughout the lungs of the animals.
