| Description | Ilaprazole (IY-81149) sodium hydrate is an orally active proton pump inhibitor that irreversibly inhibits H+/K+-ATPase in rabbit parietal cells with a dose-dependent IC50 of 6 μM. It is employed in gastric ulcer research and acts as a potent inhibitor of T-lymphokine-activated killer cell-originated protein kinase (TOPK) [1] [2]. |
| In vitro | 在组胺激活的壁细胞中，Ilaprazole (IY-81149) sodium hydrate 对14C-aminopyrine的积累表现出IC50为9 nM [1]。 |
| In vivo | Ilaprazole sodium hydrate (3-30 mg/kg；i.d.) 在剂量依赖的方式中显著抑制胃酸分泌并提高麻醉大鼠胃部pH值；组胺输注则能降低其pH值。静脉注射下，Ilaprazole sodium hydrate与Omeprazole的ED50分别为1.2 mg/kg和1.4 mg/kg；i.d.给药时分别为3.9 mg/kg和4.1 mg/kg。Ilaprazole sodium hydrate有效降低五肽胃泌素刺激的胃分泌，ED50为2.1 mg/kg，相较于Omeprazole的3.5 mg/kg。此外，Ilaprazole sodium hydrate在瘘管大鼠胃酸分泌方面展现出强效抑制作用，十二指肠内给药时其ED50为0.43 mg/kg，而Omeprazole为0.68 mg/kg。 |
| Synonyms | IY-81149 sodium hydrate |
| molecular weight | 424.45 |
| Molecular formula | C19H21N4NaO4S |
| CAS | 2322264-11-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |