| 产品描述： | Vonoprazan (TAK-438 free base), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan inhibits H+,K+-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease. Vonoprazan can be used for eradication of Helicobacter pylori |
| 靶点： |
IC50: 19 nM (porcine gastric H+,K+-ATPase, at pH 6.5) |
| 体外研究： |
Vonoprazan (0.1 nM-10 μM; 30 minutes) exhibits porcine gastric H+, K+-ATPase activity in a concentration-dependent manner. Vonoprazan does not inhibit Na+,K+-ATPase activity, even at concentrations 500 times higher than their IC50 values against gastric H+,K+-ATPase activity[ |
| 体内研究： |
Vonoprazan (1-4 mg/kg; p.o.) completely inhibits basal and 2-deoxy-D-glucose (200 mg/kg; s.c.)-stimulated gastric acid secretion at the 4 mg/kg dose in rats. Animal Model: Male 7- or 8-week-old Sprague-Dawley rat Dosage: 0.5 mg/kg, 1 mg/kg, 2 mg/kg, 4 mg/kg Administration: Oral administration Result: Inhibited basal gastric acid secretion in a dose-dependent manner. |
| 参考文献： |
1. Arikawa Y, et al. Discovery of a novel pyrrole derivative 1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine fumarate (TAK-438) as a potassium-competitive acid blocker (P-CAB). J Med Chem, 2012, 55(9), 4446-4456. 2. Hori Y, et al. 1-[5-(2-Fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine monofumarate (TAK-438), a novel and potent potassium-competitive acid blocker for the treatment of acid-related diseases. J Pharmacol Exp Ther, 2010, 335(1)(1):231-8. 3. Sugimoto M, et al. Role of Vonoprazan in Helicobacter pylori Eradication Therapy in Japan. Front Pharmacol. 2019 Jan 15;9:1560. |
| 溶解性： |
Soluble in DMSO |
| 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 |
2.895 ml |
14.476 ml |
28.953 ml |
| 5 mM |
0.579 ml |
2.895 ml |
5.791 ml |
| 10 mM |
0.29 ml |
1.448 ml |
2.895 ml |
| 50 mM |
0.058 ml |
0.29 ml |
0.579 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)
