Ilaprazole (sodium)

Ilaprazole (IY-81149) sodium is an orally active proton pump inhibitor. Ilaprazole sodium irreversibly inhibits H⁺/K⁺-ATPase in a dose-dependent manner with an IC₅₀ of 6 μM in rabbit parietal cell preparation. Ilaprazole sodium is used for the research of gastric ulcers. Ilaprazole sodium is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor^[1][2]. In Vitro:On cumulation of 14C-aminopyrine in histamine stimulated parietal cells, the IC₅₀ of Ilaprazole (IY-81149) sodium is 9 nM^[1]. In Vivo:Ilaprazole sodium (3-30 mg/kg; i.d.) dose-dependently inhibits gastric acid secretion^[1].
In anesthetized rats, Ilaprazole sodium dose-dependently increases gastric pH which is lowered by histamine infusion. In the case of i.v. injection, the ED₅₀ of Ilaprazole sodium and Omeprazole is 1.2 and 1.4 mg/kg and in the case of i.d. administration, the ED₅₀ of Ilaprazole sodium and omeprazole is 3.9 and 4.1 mg/kg, respectively. Ilaprazole sodium also significantly inhibits pentagastrin-stimulated gastric secretion. Its ED₅₀ is 2.1 mg/kg and that of Omeprazole was 3.5 mg/kg with i.d. administration. In the case of i.v. injection, Ilaprazole sodium is equipotent to Omeprazole. Ilaprazole sodium also inhibits gastric acid secretion strongly in fistular rats. The ED₅₀ of Ilaprazole sodium administered intraduodenally is 0.43 mg/kg and that of omeprazole Is 0.68 mg/kg^[1].