Ilaprazole sodium hydrate  (Synonyms: IY-81149 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^[1][2].

在组胺刺激的壁细胞中累积 14C-aminopyrine 时，Ilaprazole (IY-81149) sodium hydrate 的 IC₅₀ 为 9 nM^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Ilaprazole sodium hydrate (3-30 mg/kg；i.d.) 剂量依赖性地抑制胃酸分泌^[1]。
在麻醉大鼠中，Ilaprazole sodium hydrate 剂量依赖性地增加胃部 pH 值，而组胺输注可降低胃部 pH 值。 在静脉注射的情况下。 注射时，Ilaprazole sodium hydrate 和 Omeprazole 的 ED₅₀ 分别为 1.2 和 1.4 mg/kg，i.d. 的情况下。给药时，Ilaprazole sodium hydrate 和 Omeprazole 的 ED₅₀ 分别为 3.9 和4.1 mg/kg。Ilaprazole sodium hydrate 还显着抑制五肽胃泌素刺激的胃分泌。 其 ED₅₀ 为 2.1 mg/kg，Omeprazole 的 ED₅₀ 为 3.5 mg/kg。 在静脉注射的情况下。Ilaprazole sodium hydrate 还强烈抑制瘘管大鼠的胃酸分泌。十二指肠内给药 Ilaprazole sodium hydrate 的 ED₅₀ 为 0.43 mg/kg，Omeprazole 的 ED₅₀ 为 0.68 mg/kg^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

424.45

C₁₉H₂₁N₄NaO₄S

2322264-11-7

固体

White to light yellow

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

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

• [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.  [Content Brief]

  [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.  [Content Brief]