Ilaprazole sodium

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

艾普拉唑是一种取代的苯并咪唑前药，具有选择性和不可逆的质子泵抑制剂活性。

Ilaprazole is a substituted benzimidazole prodrug with selective and irreversible proton pump inhibitor activity. A weak base, ilaprazole accumulates in the acidic environment of the secretory canaliculus of the gastric parietal cell where it is converted to an active sulfenamide form that binds to cysteine sulfhydryl groups on the luminal aspect of the proton pump hydrogen-potassium adenosine triphosphatase (H+/K+ ATPase), thereby inhibiting the pump's activity and the parietal cell secretion of H+ ions into the gastric lumen, the final step in gastric acid production.(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 sodium (3-30 mg/kg; i.d.) dose-dependently inhibits gastric acid secretion.In anesthetized rats, Ilaprazole sodium dose-dependently increases gastric pH which is lowered by histamine infusion. In the case of i.v. injection, the ED50 of Ilaprazole sodium and Omeprazole is 1.2 and 1.4 mg/kg and in the case of i.d. administration, the ED50 of Ilaprazole sodium and omeprazole is 3.9 and 4.1 mg/kg, respectively. Ilaprazole sodium also significantly inhibits pentagastrin-stimulated gastric secretion. Its ED50 is 2.1 mg/kg and that of Omeprazole was 3.5 mg/kg with i.d. administration. In the case of i.v. injection, Ilaprazole sodium is equipotent to Omeprazole. Ilaprazole sodium also inhibits gastric acid secretion strongly in fistular rats. The ED50 of Ilaprazole sodium 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.

——

Membrane Transporter/Ion Channel

Proton Pump

Proton pump

——

——

172152-50-0

388.44

C19H17N4O2SNa

>98% (HPLC)

Soluble in DMSO

[Na+].CC1=C(C=CN=C1CS(=O)C2=NC3=C([N-]2)C=C(C=C3)N4C=CC=C4)OC

——

(-20℃)

With Ice Pack

≥ 2 years