产品说明书

Vonoprazan

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Chemical Structure| 881681-00-1 同义名 : TAK-438 free base
CAS号 : 881681-00-1
货号 : A147862
分子式 : C17H16FN3O2S
纯度 : 98%
分子量 : 345.391
MDL号 : -
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(304 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
动物实验配方：
生物活性
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.90mL

0.58mL

0.29mL

14.48mL

2.90mL

1.45mL

28.95mL

5.79mL

2.90mL
参考文献

[1]Arikawa Y, Nishida H, 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, Imanishi A, 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 Oct;335(1):231-8.

[3]Sakurai Y, Shiino M, Okamoto H, Nishimura A, Nakamura K, Hasegawa S. Pharmacokinetics and Safety of Triple Therapy with Vonoprazan, Amoxicillin, and Clarithromycin or Metronidazole: A Phase 1, Open-Label, Randomized, Crossover Study. Adv Ther. 2016;33(9):1519-1535

[4]Yang X, Li Y, Sun Y, et al. Vonoprazan: A Novel and Potent Alternative in the Treatment of Acid-Related Diseases. Dig Dis Sci. 2018;63(2):302-311

[5]Kawai T, Oda K, Funao N, et al. Vonoprazan prevents low-dose aspirin-associated ulcer recurrence: randomised phase 3 study. Gut. 2018;67(6):1033-1041