Zastaprazan, also known as JP-1366, is a proton pump inhibitor. JP-1366 mediates strong, selective, and dose-dependent inhibition of H+/K+-ATPase. JP-1366 significantly suppressed gastric acid secretion in histamine-treated pylorus-ligated rats in a dose-dependent manner. Additionally, JP-1366 inhibited histamine-stimulated gastric acid secretion in the HPD model. JP-1366 exhibited a more than 2-fold higher inhibitory effect on esophageal injury than TAK-438 in GERD lesions and had a more potent inhibitory effect in indomethacin- or aspirin-induced gastric ulcer rat models than TAK-438. Additionally, JP-1366 inhibited gastric ulcers.
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名称 | Zastaprazan |
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Iupac 化学名称 | (azetidin-1-yl)(8-{[(2,6-dimethylphenyl)methyl]amino}- 2,3-dimethylimidazo[1,2-a]pyridin-6-yl)methanone |
同义词 | Zastaprazan; JP-1366; JP 1366; JP1366; |
英文同义词 | Zastaprazan; JP-1366; JP 1366; JP1366; |
分子式 | C22H26N4O |
分子量 | 362.47 |
Smile | O=C(N1CCC1)C2=CN3C(C(NCC4=C(C)C=CC=C4C)=C2)=NC(C)=C3C |
InChiKey | FEQFUBYYZYQTOJ-UHFFFAOYSA-N |
InChi | InChI=1S/C22H26N4O/c1-14-7-5-8-15(2)19(14)12-23-20-11-18(22(27)25-9-6-10-25)13-26-17(4)16(3)24-21(20)26/h5,7-8,11,13,23H,6,9-10,12H2,1-4H3 |
Cas号 | 2133852-18-1 |
相关CAS号 |
包装 | 价格 | 库存 | 纯度 | 备货期 |
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大货 | 询价 | 询价 | 询价 |
外观性状 | 类白色固体 |
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纯度 | 98% Min. |
存储 | 0-4℃,可保存几天到几周;-20℃,可保存 几个月。 |
可溶性 | 溶于DMSO等有机溶剂 |
处理方式 | |
运输条件 | 可以在室温下进行运输。 |
海关编码 |
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Mechanism | |
Cell study | |
Animal study | |
Clinical study |
1: Ku JM, Cho JH, Kim K, Kim JY, Kim JY, Kim J, Cha H, Cheon B. JP-1366: A novel and potent potassium-competitive acid blocker that is effective in the treatment of acid-related diseases. Pharmacol Res Perspect. 2023 Jun;11(3):e01090. doi: 10.1002/prp2.1090. PMID: 37147903; PMCID: PMC10163344.
2: Hwang I, Ji SC, Oh J, Kim H, Cha H, Kim J, Lee CS, Yu KS, Lee S. Randomised clinical trial: Safety, tolerability, pharmacodynamics and pharmacokinetics of zastaprazan (JP-1366), a novel potassium-competitive acid blocker, in healthy subjects. Aliment Pharmacol Ther. 2023 Apr;57(7):763-772. doi: 10.1111/apt.17406. Epub 2023 Feb 2. PMID: 36732884.