CS-526

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[1].

Research Areas >> Inflammation/Immunology

Signaling Pathways >> Membrane Transporter/Ion Channel >> Proton Pump

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[1]。 CS-526 竞争性结合 H+ K+-ATPase 的 K+ 结合位点[1]。

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[1]。 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[1]。 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[1]。 Animal Model: Pylorus-Ligated Rats[1] 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[1] 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.

[1]. Ito K, et al. Pharmacological profile of novel acid pump antagonist 7-(4-fluorobenzyloxy)-2,3-dimethyl-1-{[(1S,2S)-2-methyl cyclopropyl]methyl}-1H-pyrrolo[2,3-d]pyridazine (CS-526). J Pharmacol Exp Ther. 2007 Oct;323(1):308-17.