| Bioactivity | 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]. |
| Invitro | 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]。 |
| In Vivo | 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: |
| Name | CS-526 |
| CAS | 313272-12-7 |
| Formula | C20H22FN3O |
| Molar Mass | 339.41 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |