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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Proton Pump-Zastaprazan
Zastaprazan

Chemical Structure : Zastaprazan

CAS No.: 2133852-18-1

Zastaprazan (JP-1366, JP1366)

货号: PC-38430Not For Human Use, Lab Use Only.

Zastaprazan (JP-1366) is a potent selective inhibitor of gastric H+/K+-ATPase activity with IC50 of 16.7 nM, >400-fold selectivity over Na+/K+-ATPase activity.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Zastaprazan (JP-1366) is a potent selective inhibitor of gastric H+/K+-ATPase activity with IC50 of 16.7 nM, >400-fold selectivity over Na+/K+-ATPase activity.
JP-1366 (2 mg/kg) inhibits basal and histamine-stimulated gastric acid secretion in pylorus-ligated rats.
JP-1366 inhibits esophageal mucosal damage in a reflux esophagitis model with ED50 of 0.53 mg/kg.
JP-1366 exhibits a more than 2-fold higher inhibitory effect on esophageal injury than TAK-438 in GERD lesions and has a more potent inhibitory effect in indomethacin- or aspirin-induced gastric ulcer rat models than TAK-438.

物理化学性质&存储条件

分子量 362.477
分子式 C22H26N4O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

azetidin-1-yl(8-((2,6-dimethylbenzyl)amino)-2,3-dimethylimidazo[1,2-a]pyridin-6-yl)methanone

参考文献

1. Jin Mo Ku, et al. Pharmacol Res Perspect. 2023 Jun;11(3):e01090.

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