| 产品描述： | 选择性H +，K + -ATPase抑制剂;Selective H+,K+-ATPase inhibitor;PF-3716556是一种有效的，选择性的P-CAB钾离子竞争性酸抑制剂，在离子渗透和离子密集检测中，抑制猪H+，K+-ATPase活性，抑制胃酸分泌，对Na+，K+-ATPas没有作用活性，用于治疗胃食管返流疾病。;PF 3716556 is a potent and selective P-CAB (potassium-competitive acid blocker), with pIC50 of 6.026 and 7.095 for the inhibition of porcine H+,K+-ATPase activity in ion-leaky and ion-tight assay, respectively, inhibits gastric acid secretion, displays no activity at Na+,K+-ATPase, used for the treatment of gastroesophageal reflux disease.A highly selective H+,K+-ATPase inhibitor that is more potent in acidic conditions. |
| 靶点： |
pIC50: 6.026 (Porcine gastric H+,K+-ATPase), 6.038 (Canine gastric H+,K+-ATPase) and 6.009 (Recombinant gastric H+,K+-ATPase) |
| 体内研究： |
PF 03716556 (1-10 mg/kg；十二指肠内给药；一次；雄性 Sprague-Dawley 大鼠) 处理以剂量依赖性方式抑制大鼠胃酸分泌。 |
| 参考文献： |
1. Hiroki Mori, 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. |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.535 ml |
12.675 ml |
25.35 ml |
| 5 mM |
0.507 ml |
2.535 ml |
5.07 ml |
| 10 mM |
0.254 ml |
1.268 ml |
2.535 ml |
| 50 mM |
0.051 ml |
0.254 ml |
0.507 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京