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Tenatoprazole
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Tenatoprazole图片
CAS NO:113712-98-4
包装:50mg
规格:98%
市场价:604元
分子量:346.4

产品介绍
proton pump inhibitor
CAS:113712-98-4
分子式:C16H18N4O3S
分子量:346.4
纯度:98%
存储:Store at -20°C

Background:

Tenatoprazole sodium (TU-199 sodium) is a proton pump inhibitor; inhibits hog gastric H+/K+-ATPase with an IC50 of 6.2 μM.


Tenatoprazole inhibits hog gastric H+/K+-ATPase activity with almost equal potency to that of omeprazole (IC50=6.2 and 4.2 microM, respectively)[1]. Tenatoprazole is a prodrug of the proton pump inhibitor class. Tenatoprazole is converted to the active sulfenamide or sulfenic acid by acid in the secretory canaliculus of the stimulated parietal cell of the stomach. This active species binds to luminally accessible cysteines of the gastric H+/K+-ATPase resulting in disulfide formation and acid secretion inhibition. Tenatoprazole binds at the catalytic subunit of the gastric acid pump with a stoichiometry of 2.6 nmol/mg of the enzyme[2].


Tenatoprazole inhibits basal gastric acid secretion in pylorus-ligated rats in a dose-dependent manner (ED50=4.2 mg/kg p.o.). In gastric fistula rats, tenatoprazole (2.5 and 5 mg/kg i.d.) also inhibits gastric acid secretion stimulated by histamine, carbachol or tetragastrin. Furthermore, tenatoprazole prevents the formation of water-immersion restraint stress-, pylorus ligation- and indomethacin-induced gastric lesions, and mepirizole-induced duodenal ulcer in rats[1]. Maximum binding of tenatoprazole is 2.9 nmol/mg of the enzyme at 2 h after IV administration. The binding sites of tenatoprazole are in the TM5/6 region at Cys813 and Cys822. The bioavailability of tenatoprazole is two-fold greater in the (S)-tenatoprazole sodium salt hydrate form as compared to the free form in dogs[2].


参考文献:
[1]. Shin JM, et al. Characterization of the inhibitory activity of tenatoprazole on the gastric H+,K+ -ATPase in vitro and in vivo. Biochem Pharmacol. 2006 Mar 14;71(6):837-49.
[2]. https://www.ncbi.nlm.nih.gov/pubmed/16405921