Ilaprazole sodium hydrate

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.

On cumulation of 14C-aminopyrine in histamine stimulated parietal cells, the IC₅₀ of Ilaprazole (IY-81149) sodium hydrate is 9 nM^[1].

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].

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.
[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.