产品
编 号:F751275
分子式:C19H21N4NaO4S
分子量:424.45
产品类型
结构图
CAS No: 2322264-11-7
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生物活性:
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.
体内研究:
Ilaprazole sodium hydrate (3-30 mg/kg;i.d.) 剂量依赖性地抑制胃酸分泌。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。Animal Model:Male SD rat (after pylorus ligation)
Dosage:3, 10, 30 mg/kg
Administration:Intraduodenally
Result:The acid output and volume significantly inhibited by about 60% and 46% at 3 mg/kg were s, respectively. At 30 mg/kg, it showed 93% and 73% inhibition on acid output and volume, respectively.
体外研究:
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。