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PF 03716556

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Chemical Structure| 928774-43-0 同义名 : PF-3716556
CAS号 : 928774-43-0
货号 : A597315
分子式 : C22H26N4O3
纯度 : 98%
分子量 : 394.467
MDL号 : MFCD19690947
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 20 mg/mL(50.7 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • ATPase

    H+/K+-ATPase, pIC50:~6.5

  • Proton Pump

    H+/K+-ATPase, pIC50:~6.5
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.54mL

0.51mL

0.25mL

12.68mL

2.54mL

1.27mL

25.35mL

5.07mL

2.54mL
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