Ilaprazole (IY-81149) sodium，一种具有口服活性质子泵抑制剂，以剂量依赖性方式不可逆地抑制H⁺/K⁺-ATPase，在兔壁细胞制剂中的 IC₅₀ 为 6 μM。Ilaprazole sodium 用于胃溃疡的研究。Ilaprazole sodium 也是一种有效的T细胞起源蛋白激酶 (TOPK) 抑制剂。

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 IC 50 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.

Solid

On cumulation of 14C-aminopyrine in histamine stimulated parietal cells, the IC50 of Ilaprazole (IY-81149) sodium is 9 nM. has not independently confirmed the accuracy of these methods. They are for reference only.

Ilaprazole sodium (3-30 mg/kg; i.d.) dose-dependently inhibits gastric acid secretion.
In anesthetized rats, Ilaprazole sodium dose-dependently increases gastric pH which is lowered by histamine infusion. In the case of i.v. injection, the ED 50 of Ilaprazole sodium and Omeprazole is 1.2 and 1.4 mg/kg and in the case of i.d. administration, the ED 50 of Ilaprazole sodium and omeprazole is 3.9 and 4.1 mg/kg, respectively. Ilaprazole sodium also significantly inhibits pentagastrin-stimulated gastric secretion. Its ED 50 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.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

[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.

In Vitro: DMSO : 41.67 mg/mL (107.28 mM; Need ultrasonic)配制储备液