产品说明书
Vonoprazan Fumarate
 |
同义名 : | TAK-438 |
| CAS号 : | 881681-01-2 | |
| 货号 : | A108580 | |
| 分子式 : | C21H20FN3O6S | |
| 纯度 : | 98% | |
| 分子量 : | 461.463 | |
| MDL号 : | MFCD18633280 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,Room temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 50 mg/mL(108.35 mM)，配合低频超声助溶，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 |
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| 动物实验配方： |
0.5% methylcellulose+water 17 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 描述 | The potassium-competitive acid blocker (P-CAB), a new class of acid suppressant, inhibits gastric H+,K+-ATPase activity by reversible and K+-competitive ionic binding to the enzyme. TAK-438 is a novel P-CAB that reversibly inhibits H+,K+-ATPase with IC50 of 19 nM (pH 6.5), and exhibits potent gastric acid secretion inhibitory action in vivo. And TAK-438 was selected as a drug candidate for the treatment of gastroesophageal reflux disease (GERD), peptic ulcer, and other acid-related diseases [3]. Under weakly acidic conditions (pH 6.5), TAK-438 inhibited gastric H+,K+-ATPase activity in a concentration-dependent manner. Under neutral conditions (pH 7.5), the inhibitory activity of TAK-438 was almost the same as that under weakly acidic conditions. In Pylorus-Ligated rats, TAK-438 at doses of 0.5, 1, 2, and 4 mg/kg inhibited basal gastric acid secretion in a dose-dependent manner, and the ID50 value was 1.26 mg/kg. In Anesthetized rats, TAK-438 inhibited 2DG-stimulated gastric acid secretion in a dose-dependent manner, and the ID50 value of TAK-438 was 0.83 mg/kg. TAK-438 completely inhibited gastric acid secretion at the 4 mg/kg dose [4]. | ||
| 作用机制 | TAK-438 inhibited gastric H+,K+-ATPase in a K+-competitive manner [4]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.17mL 0.43mL 0.22mL |
10.84mL 2.17mL 1.08mL |
21.67mL 4.33mL 2.17mL |
| 参考文献 |
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