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PF 3716556_分子结构_CAS_928774-43-0)
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PF 3716556

产品号 S2222 公司名称 Selleck Chemicals
CAS号 928774-43-0 公司网站 http://www.selleckchem.com
分子式 C22H26N4O3 电 话 (877) 796-6397
分子量 394.46684 传 真 (832) 582-8590
纯 度 电子邮件 sales@selleckchem.com
保 存 -20°C Chembase数据库ID: 72830

产品价格信息

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产品别名

标题
PF 3716556
IUPAC标准名
N-(2-hydroxyethyl)-N,2-dimethyl-8-{[(4R)-5-methyl-3,4-dihydro-2H-1-benzopyran-4-yl]amino}imidazo[1,2-a]pyridine-6-carboxamide
IUPAC传统名
N-(2-hydroxyethyl)-N,2-dimethyl-8-{[(4R)-5-methyl-3,4-dihydro-2H-1-benzopyran-4-yl]amino}imidazo[1,2-a]pyridine-6-carboxamide
别名
PF-3716556
PF-03716556

产品登记号

CAS号 928774-43-0

产品性质

作用靶点 ATPase
成盐信息 Free Base
保存条件 -20°C

产品详细信息

详细说明 (English)
Research Area: Cancer
Biological Activity:
PF-03716556 is a potent, and selective acid pump antagonist with pIC50 of 6.026 ± 0.112, 6.038 ± 0.039 and 6.009 ± 0.209 at pH 6.4 for the inhibition of H+, K+-ATPase activity of porcine, canine and human ion-leaky membrane vesicles, respectively.PF-03716556 is used for the treatment of gastroesophageal reflux disease. PF-03716556 is highly selective for H+, K+-ATPase in vitro. PF-03716556 displays no activity at Na+, K+-ATPase. PF-03716556 inhibits gastric acid secretion in rat and dog models. PF-03716556 has no species differences among the porcine, canine and human enzymes. PF-03716556 produced greater inhibition than revaprazan in both the in vitro (ion-tight assay) and in vivo conditions. PF-03716556 offers long-lasting and maximal efficacy within 30 min of a single dosing with responses that are maintained for at least 5 days of repeated dosing with no signs of tolerance. PF-03716556 did not exhibit any biologically relevant activity against any of the tested more than 50 (e.g., adenosine receptor) receptors, ion channels, or enzymes expressed in naïve tissues, cell lines and transfectants. [1]References on PF 3716556[1] J Pharmacol Exp Ther., 2009 Feb, 328(2):671-9.

参考文献

  • Mori H et al. J Pharmacol Exp Ther. 2009 Feb;328(2):671-9.