|(R)-N-(2-羟乙基)-N,2-二甲基-8-((5-甲基苯并吡喃-4-基)氨基)咪唑并[1,2-a]吡啶-6-甲酰胺|CsnPharm

CAS No.: 928774-43-0

(R)-N-(2-Hydroxyethyl)-N,2-dimethyl-8-((5-methylchroman-4-yl)amino)imidazo[1,2-a]pyridine-6-carboxamide Catalog No. CSN17177

Synonyms: PF-3716556

PF 03716556 is a selective H+,K+ ATPase inhibitor with pIC50 value of 6.009.

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实验方案

技术信息

生物活性

描述The gastric H⁺,K⁺-ATPase, which is responsible for gastric acid secretion, is a P₂-type ATPase located in the apical membrane of parietal cells. PF-03716556 is a novel, potent, and selective acid pump antagonist. In the ion-leaky membranes of porcine vesicles, canine vesicles and human recombinant cells, F-03716556 inhibited H⁺,K⁺-ATPase activity with pIC₅₀ values of 6.026±0.112, 6.038±0.039 and 6.009±0.209 at pH 6.4, respectively. In the ion-tight membrane of porcine vesicles, PF-03716556 inhibited H⁺,K⁺-ATPase activity in a concentration-dependent manner, with a pIC₅₀ value of 7.095±0.077 at pH 7.4. PF-03716556 exhibited high selectivity for the H⁺,K⁺-ATPase over the Na⁺,K⁺-ATPase. In vivo, administration of PF-03716556 inhibited gastric acid secretion in a dose-dependent manner over concentrations ranging from 1 to 10 mg/kg in Ghosh-Schild rats and 0.3 to 3 mg/kg in Heidenhain Pouch Dogs, respectively^[2].
参考文献

[1] Mori H, Tonai-Kachi H, et al. N-(2-hydroxyethyl)-N,2-dimethyl-8-{[(4R)-5-methyl-3,4-dihydro-2H-chromen-4-yl] amino}imidazo[1,2-a] pyridine-6-carboxamide (PF-03716556), a novel, potent, and selective acid pump antagonist for the treatment of gastroesophageal reflux disease. J Pharmacol Exp Ther. 2009 Feb;328(2):671-9.
[2] Mori H, Tonai-Kachi H, et al. N-(2-hydroxyethyl)-N,2-dimethyl-8-{[(4R)-5-methyl-3,4-dihydro-2H-chromen-4-yl]amino}imidazo[1,2-a]pyridine-6-carboxamide (PF-03716556), a novel, potent, and selective acid pump antagonist for the treatment of gastroesophageal reflux disease. J Pharmacol Exp Ther. 2009 Feb;328(2):671-9

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5351 mL
- 12.6753 mL
- 25.3507 mL
- 5 mM
- 0.5070 mL
- 2.5351 mL
- 5.0701 mL
- 10 mM
- 0.2535 mL
- 1.2675 mL
- 2.5351 mL

技术信息

CAS号

928774-43-0

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H26N4O3

运输

蓝冰

分子量

394.47

别名

PF-3716556

溶解度

DMSO	200.0 mg/mL (507.0 mM)
Water	insoluble

动物实验配方

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(R)-N-(2-Hydroxyethyl)-N,2-dimethyl-8-((5-methylchroman-4-yl)amino)imidazo[1,2-a]pyridine-6-carboxamide Catalog No. CSN17177

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