产品
编 号:F495677
分子式:C17H16FN3O2S
分子量:345.39
产品类型
结构图
CAS No: 881681-00-1
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产品详情
生物活性:
Vonoprazan (TAK-438 free base), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan inhibits H+,K+-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease. Vonoprazan can be used for eradication of Helicobacter pylori.
体内研究:
Vonoprazan (1-4 mg/kg; p.o.) completely inhibits basal and 2-deoxy-D-glucose (200 mg/kg; s.c.)-stimulated gastric acid secretion at the 4 mg/kg dose in rats.Animal Model:Male 7- or 8-week-old Sprague-Dawley rat
Dosage:0.5 mg/kg, 1 mg/kg, 2 mg/kg, 4 mg/kg
Administration:Oral administration
Result:Inhibited basal gastric acid secretion in a dose-dependent manner.
体外研究:
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 IC50 values against gastric H+,K+-ATPase activity.