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Ilaprazole

CAS No. : 172152-36-2

MCE 国际站：Ilaprazole

产品活性：Ilaprazole (IY-81149)，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 用于胃溃疡的研究。Ilaprazole 也是一种有效的T细胞起源蛋白激酶 (TOPK) 抑制剂。

研究领域：Membrane Transporter/Ion Channel  |  Cell Cycle/DNA Damage

作用靶点：Proton Pump  |  TOPK

In Vitro: On cumulation of 14C-aminopyrine in histamine stimulated parietal cells, the IC₅₀ of Ilaprazole (IY-81149) sodium is 9 nM.

In Vivo: Ilaprazole (3-30 mg/kg; i.d.) dose-dependently inhibits gastric acid secretion.
In anesthetized rats, Ilaprazole dose-dependently increased gastric pH which was lowered by histamine infusion. In the case of i.v. injection, the ED₅₀ of Ilaprazole and omeprazole is 1.2 and 1.4 mg/kg and in the case of i.d. administration, the ED₅₀ of Ilaprazole and omeprazole is 3.9 and 4.1 mg/kg, respectively. Ilaprazole also significantly inhibits pentagastrin-stimulated gastric secretion. Its ED₅₀ is 2.1 mg/kg and that of Omeprazole is 3.5 mg/kg with i.d. administration. In the case of i.v. injection, Ilaprazole is equipotent to Omeprazole. Ilaprazole also inhibits gastric acid secretion strongly in fistular rats. The ED₅₀ of Ilaprazole administered intraduodenally is 0.43 mg/kg and that of Omeprazole is 0.68 mg/kg.

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