产品
编 号:F315685
分子式:C20H22FN3O
分子量:339.41
产品类型
结构图
CAS No: 313272-12-7
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产品详情
生物活性:
CS-526 is a potent, selective, reversible and orally active acid pump antagonist. CS-526 inhibits H+,K+-ATPase activity. CS-526 inhibits gastric acid secretion and prevents esophageal lesions. CS-526 has the potential for the research of gastroesophageal reflux disease.
体内研究:
CS-526 (1, 3, 10, 30 mg/kg; intraduodenal or p.o.) 以剂量依赖性方式抑制幽门结扎大鼠的胃酸分泌。CS-526 (1, 3, 10, 30 mg/kg; intrapouch; 180 min) 剂量依赖性地抑制 Heidenhain 袋犬组胺诱导的胃酸分泌。CS-526 (1, 3, 10, 30 mg/kg; intraduodenal or p.o.) 可预防食管病变和急性胃粘膜病变。Animal Model:Pylorus-Ligated Rats
Dosage:1, 3, 10, 30 mg/kg
Administration:Intraduodenal administration or p.o.
Result:Dose-dependently inhibited gastric acid secretion with ID50 values of 2.8, 0.7 mg/kg for intraduodenal administration and oral administration, respectively.
Animal Model:Reflux Esophagitis Model in Rats
Dosage:1, 3, 10 mg/kg
Administration:Intraduodenal administration or p.o.
Result:Significantly reduced the lesion scores with ID50 values of 5.4, 1.9 mg/kg for intraduodenal and p.o. respectively.
体外研究:
CS-526 (0-100 μM;60 分钟) 抑制 H+ K+-ATP 酶和 Na+ K+ -ATPase 活性呈剂量依赖性,IC50 值分别为 61 nM、10.4 μM。CS-526 竞争性结合 H+ K+-ATPase 的 K+ 结合位点。