313272-12-7

313272-12-7 structure

Name: CS-526
Chemical Name: 7-(4-fluorobenzyloxy)-2,3-dimethyl-1-{[(1S,2S)-2-methylcyclopropyl]methyl}-1H-pyrrolo[2,3-d]pyridazine
CAS Number: 313272-12-7
Molecular Formula: C₂₀H₂₂FN₃O
Molecular Weight: 339.41
Create Date: 2018-01-20 19:15:01
Modify Date: 2024-01-29 16:08:11
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].

Name	7-(4-fluorobenzyloxy)-2,3-dimethyl-1-{[(1S,2S)-2-methylcyclopropyl]methyl}-1H-pyrrolo[2,3-d]pyridazine
Synonyms	7-(4-fluorobenzyloxy)-2,3-dimethyl-1-[(1S,2S)-2-methylcyclopropylmethyl]pyrrolo[2,3-d]pyridazine CS-526

Description	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].
Related Catalog	Research Areas >> Inflammation/Immunology Signaling Pathways >> Membrane Transporter/Ion Channel >> Proton Pump
In Vitro	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: 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.

Molecular Formula	C₂₀H₂₂FN₃O
Molecular Weight	339.41
Exact Mass	339.17500
PSA	39.94000
LogP	4.42220

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