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CAS No.: 881681-00-1

沃诺拉赞 Catalog No. CSN18522

Synonyms: TAK-438 free base;TAK-438;沃诺拉赞

TAK-438 Free Base is a blocker of potassium-competitive proton pump that reversibly inhibits H+/K+ ATPase with IC50 of 17 nM at pH 6.5 while do not affect on Na+/K+ ATPase activity. It has been used to treatment of erosive esophagitis and gastroduodenal ulcer.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 H+/K+ ATPase

IC50:19nM(pH6.5)
描述TAK-438 free base (Vonoprazan) is an orally active potassium-competitive acid blocker which inhibits H+, K+-ATPase activity with an IC50 of 19 nM. It is a novel potassium-competitive acid blocker that inhibits gastric H(+), K(+)-ATPase. In healthy Japanese male subjects, triple therapy with vonoprazan-amoxicillin-clarithromycin increased vonoprazan and clarithromycin exposure. The safety and tolerability profile of triple therapy with vonoprazan-amoxicillin-clarithromycin or vonoprazan-amoxicillin-metronidazole was favorable in this population^[3]. The healing rate of GERD (gastroesophageal reflux disease) and gastric ulcers by vonoprazan is more than 95 and 90%, respectively; also, it is effective in curing PPI (proton pump inhibitors)-resistant GERD. It is also effective in the eradication of clarithromycin-resistant H. pylori strains. All of these short-term studies show vonoprazan is safe and well-tolerated^[4]. Vonoprazan (10 and 20 mg) was as effective as lansoprazole (15 mg) in preventing peptic ulcer recurrence during LDA (low-dose aspirin) therapy, had a similar long-term safety profile and was well tolerated^[5].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03085836	Healthy Participants	Phase 1	Completed	-	China ... more >> Zhongshan Hospital Fudan University Shanghai, China, 200032 Collapse <<
NCT03456960	Japanese Healthy Adult Male	Phase 1	Completed	-	Japan ... more >> Fukuoka Mirai Hospital Fukuoka, Japan Collapse <<

参考文献

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
- 2.8953 mL
- 14.4763 mL
- 28.9527 mL
- 5 mM
- 0.5791 mL
- 2.8953 mL
- 5.7905 mL
- 10 mM
- 0.2895 mL
- 1.4476 mL
- 2.8953 mL

技术信息

CAS号

881681-00-1

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H16FN3O2S

运输

蓝冰

分子量

345.39

别名

TAK-438 free base;TAK-438;沃诺拉赞

溶解度

DMSO	210.0 mg/mL (608.0 mM)
Water	insoluble

动物实验配方

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