Vonoprazan Fumarate

Vonoprazan Fumarate (TAK-438), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB) , with antisecretory activity. Vonoprazan Fumarate inhibits H + ,K + -ATPase activity in porcine gastric microsomes with an IC 50 of 19 nM at pH 6.5. Vonoprazan Fumarate is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease In Vitro Vonoprazan (0.1 nM-10 μM; 30 minutes) exhibits porcine gastric H + ,K + -ATPase activity in a concentration-dependent manner. Vonoprazan does not inhibit Na + ,K + -ATPase activity, even at concentrations 500 times higher than their IC 50 values against gastric H + ,K + -ATPase activity. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo Vonoprazan (1-4 mg/kg; p.o.) completely inhibits basal and 2-deoxy-D-glucose (2DG, 200 mg/kg s.c.)-stimulated gastric acid secretion at the 4 mg/kg dose in rats. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male 7- or 8-week-old Sprague-Dawley ratDosage: 0.5, 1, 2, and 4 mg/kg Administration: Oral administration Result: Inhibited basal gastric acid secretion in a dose-dependent manner. IC50& Target:IC50: 19 nM (porcine gastric H + ,K + -ATPase, at pH 6.5)

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