161796-84-5
中文名稱
艾美拉唑鉀鹽
英文名稱
Esomeprazole potassium
CAS
161796-84-5
分子式
C17H19KN3O3S
分子量
384.51
MOL 文件
161796-84-5.mol
161796-84-5 結(jié)構(gòu)式
基本信息
中文別名
埃索拉唑鉀鹽埃索美拉唑鉀
艾美拉唑鉀鹽
埃索美拉唑鉀鹽
6-甲氧基-2-[(S)-[(4-甲氧基-3,5-二甲基-2-吡啶基)甲基]亞磺?；鵠-1H-苯并咪唑鉀鹽
6-甲氧基-2-[(S)-[(4-甲氧基-3,5-二甲基-2-吡啶基)甲基]亞磺?；鵠-1H-苯并咪唑鉀鹽 (1:1)
英文別名
Esomeprazole potassium(S)-Omeprazole potassium
Esomeprazole potassium USP/EP/BP
(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
(R)-5-METHOXY-2-((4-METHOXY-3,5-DIMETHYLPYRIDIN-2-YL)METHYLSULFINYL)BENZO[D]IMIDAZOL-1-IDE POTASSIUM SALT
6-Methoxy-2-[(S)-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole potassium salt (1:1)
1H-Benzimidazole,6-methoxy-2-[(S)-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-,potassium salt (1:1)
所屬類別
原料藥：抑制劑
常見問題列表
概述
艾美拉唑鉀鹽是一種質(zhì)子泵抑制劑，艾美拉唑鉀鹽是奧美拉唑的S-異構(gòu)體，通過特異性的質(zhì)子泵抑制作用減少胃酸分泌，奧美拉唑的R-異構(gòu)體和S-異構(gòu)體具有相似的藥效學(xué)特性。艾美拉唑鉀鹽為弱堿性藥物，在壁細胞泌酸微管的高酸環(huán)境中濃集并轉(zhuǎn)化為活性形式，從而抑制該部位的H+/K+-ATP酶(質(zhì)子泵)，對基礎(chǔ)胃酸分泌和受刺激后的胃酸分泌均產(chǎn)生抑制。應(yīng)用
艾美拉唑鉀鹽鹽是通過艾美拉唑鉀鹽成鹽得到的，艾美拉唑鉀鹽鹽能夠降低對機體的刺激性，并且在機體中具有良好的溶解性，提高生物利用度，從而能夠產(chǎn)生更理想的藥理作用，常見的艾美拉唑鉀鹽鹽主要有艾美拉唑鉀鹽鈉鹽、艾美拉唑鉀鹽鉀鹽、艾美拉唑鉀鹽鎂鹽。目前，艾美拉唑鉀鹽鹽主要通過艾美拉唑鉀鹽成鹽得到，因此，艾美拉唑鉀鹽的制備方法不僅影響艾美拉唑鉀鹽的純度，而且影響艾美拉唑鉀鹽鹽的純度。生物活性
Esomeprazole potassium salt ((S)-Omeprazole potassium salt) 是一種有效的具有口服活性質(zhì)子泵抑制劑，可通過抑制胃壁細胞中的 H+, K+-ATPase 來降低酸分泌，并可用于胃食管反流疾病的研究。靶點
H + , K + -ATPase
體外研究
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. |
體內(nèi)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. |