Ilaprazole

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的口服活性质子泵抑制剂，不可逆地抑制 H+/K(+)-ATPase，IC50 为 6 uM。

A potent, orally active proton pump inhibitor that irreversibly inhibits H+/K(+)-ATPase with IC50 of 6 uM; dose-dependently increases gastric pH in anesthetized rats, exhibits superior potency against gastric acid secretion compared with omeprazole.Ulcer Approved.

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

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. 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.

IY81149 | IY-81149 | IY 81149

Membrane Transporter/Ion Channel

Proton Pump

Proton Pump

Other Indications

Ulcer

172152-36-2

366.43682

C19H18N4O2S

>98% (HPLC)

DMSO: ≥ 35 mg/mL

O=S(C1=NC2=CC(N3C=CC=C3)=CC=C2N1)CC4=NC=CC(OC)=C4C

1H-Benzimidazole, 2-[[(4-methoxy-3-methyl-2-pyridinyl)methyl]sulfinyl]-6-(1H-pyrrol-1-yl)-

(-20℃)

With Ice Pack

≥ 2 years