| Identification | Back Directory | [Name]
1H-Benzimidazole, 2-[[(4-methoxy-3-methyl-2-pyridinyl)methyl]sulfinyl]-6-(1H-pyrrol-1-yl)-, sodium salt, hydrate (1:1:2) | [CAS]
2322264-11-7 | [Synonyms]
Ilaprazole sodium hydrate
1H-Benzimidazole, 2-[[(4-methoxy-3-methyl-2-pyridinyl)methyl]sulfinyl]-6-(1H-pyrrol-1-yl)-, sodium salt, hydrate (1:1:2) | [Molecular Formula]
C19H21N4NaO3S | [MOL File]
2322264-11-7.mol | [Molecular Weight]
408.45 |
| Hazard Information | Back Directory | [Uses]
Ilaprazole (IY-81149) sodium hydrate is an orally active proton pump inhibitor. Ilaprazole sodium hydrate irreversibly inhibits H+/K+-ATPase in a dose-dependent manner with an IC50 of 6 μM in rabbit parietal cell preparation. Ilaprazole sodium hydrate is used for the research of gastric ulcers. Ilaprazole sodium hydrate is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor[1][2]. | [in vivo]
Ilaprazole sodium hydrate (3-30 mg/kg; i.d.) dose-dependently inhibits gastric acid secretion[1].
In anesthetized rats, Ilaprazole sodium hydrate dose-dependently increases gastric pH which is lowered by histamine infusion. In the case of i.v. injection, the ED50 of Ilaprazole sodium hydrate and Omeprazole is 1.2 and 1.4 mg/kg and in the case of i.d. administration, the ED50 of Ilaprazole sodium hydrate and omeprazole is 3.9 and 4.1 mg/kg, respectively. Ilaprazole sodium hydrate also significantly inhibits pentagastrin-stimulated gastric secretion. Its ED50 is 2.1 mg/kg and that of Omeprazole is 3.5 mg/kg with i.d. administration. In the case of i.v. injection, Ilaprazole sodium hydrate is equipotent to Omeprazole. Ilaprazole sodium hydrate also inhibits gastric acid secretion strongly in fistular rats. The ED50 of Ilaprazole sodium hydrate administered intraduodenally is 0.43 mg/kg and that of Omeprazole Is 0.68 mg/kg[1]. | Animal Model: | Male SD rat (after pylorus ligation)[1] | | Dosage: | 3, 10, 30 mg/kg | | Administration: | Intraduodenally | | Result: | The acid output and volume significantly inhibited by about 60% and 46% at 3 mg/kg were s, respectively. At 30 mg/kg, it showed 93% and 73% inhibition on acid output and volume, respectively. |
| [References]
[1] Kwon D, et al. Effects of IY-81149, a newly developed proton pump inhibitor, on gastric acid secretion in vitro and in vivo. Arzneimittelforschung. 2001;51(3):204-213. DOI:10.1055/s-0031-1300026
[2] Zheng M, et al. Proton pump inhibitor ilaprazole suppresses cancer growth by targeting T-cell-originated protein kinase. Oncotarget. 2017;8(24):39143-39153. DOI:10.18632/oncotarget.16609 |
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