| Identification | Back Directory | [Name]
R 105266) | [CAS]
313272-12-7 | [Synonyms]
AKU 517
R 105266)
CS526,CS 526
CS-526
(AKU 517
1H-Pyrrolo[2,3-d]pyridazine, 7-[(4-fluorophenyl)methoxy]-2,3-dimethyl-1-[[(1S,2S)-2-methylcyclopropyl]methyl]- | [Molecular Formula]
C20H22FN3O | [MDL Number]
MFCD16628172 | [MOL File]
313272-12-7.mol | [Molecular Weight]
339.41 |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
CS-526 (1, 3, 10, 30 mg/kg; intraduodenal or p.o.) inhibits gastric acid secretion in a dose-dependent manner in pylorus-ligated rats[1].
CS-526 (1, 3, 10, 30 mg/kg; intrapouch; 180 min) dose-dependently inhibits the histamine-induced gastric acid secretion in the Heidenhain pouch dogs[1].
CS-526 (1, 3, 10, 30 mg/kg; intraduodenal or p.o.) prevents esophageal lesions and acute gastric mucosal lesions[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. |
| [References]
[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. DOI:10.1124/jpet.107.121350 |
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