Vonoprazan Fumarate 是质子泵的有效抑制剂，是口服有效的高效钾竞争性酸阻断剂，具有抗分泌活性。在 pH 为 6.5 时，它抑制猪胃微粒体中的 H+,K+-ATPase 酶活性，IC50为 19 nM。它被开发用于研究酸相关疾病，如消化性溃疡和胃食管反流病。

Vonoprazan Fumurate, a novel potassium-competitive acid blocker, inhibits gastric acid secretion. Vonoprazan Fumurate inhibited H+,K+-ATPase activity in porcine gastric microsomes with IC50 value of 19 nM at pH 6.5.

The inhibitory activity of Vonoprazan Fumurate was unaffected by ambient pH. The inhibition by Vonoprazan Fumurate was reversible and achieved in a K(+)-competitive manner, quite different from that by lansoprazole. Vonoprazan Fumurate exhibits porcine gastric H+ ,K+-ATPase activity in a concentration-dependent manner[4].

Vonoprazan Fumurate, at a dose of 4 mg/kg (as the free base) orally, completely inhibited basal and 2-deoxy-d-glucose-stimulated gastric acid secretion in rats, and its effect on both was stronger than that of lansoprazole. Vonoprazan Fumurate increased the pH of gastric perfusate to a higher value than did lansoprazole or SCH28080, and the effect of Vonoprazan Fumurate was sustained longer than that of lansoprazole or SCH28080[4].

881681-01-2

C21H20FN3O6S

461.46

富马酸沃诺拉赞;Vonoprazan Fumurate;TAK-438;TAK438;TAK 438

DMSO:Soluble
Powder: -20°C for 3 years
In solvent: -80°C for 2 years