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Tenatoprazole sodium

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产品编号 T61445Cas号 335299-59-7

Tenatoprazole sodium (TU-199 sodium) is a potent proton pump inhibitor that effectively suppresses the activity of hog gastric H+/K+-ATPase, a vital enzymatic pump involved in acid secretion. It achieves this inhibition at an impressive IC50 value of 6.2 μM.

Tenatoprazole sodium

Tenatoprazole sodium

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产品编号 T61445Cas号 335299-59-7

Tenatoprazole sodium (TU-199 sodium) is a potent proton pump inhibitor that effectively suppresses the activity of hog gastric H+/K+-ATPase, a vital enzymatic pump involved in acid secretion. It achieves this inhibition at an impressive IC50 value of 6.2 μM.

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25 mg¥ 10,6001-2周
50 mg¥ 13,8001-2周
100 mg¥ 17,5001-2周
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产品介绍

生物活性
产品描述
Tenatoprazole sodium (TU-199 sodium) is a potent proton pump inhibitor that effectively suppresses the activity of hog gastric H+/K+-ATPase, a vital enzymatic pump involved in acid secretion. It achieves this inhibition at an impressive IC50 value of 6.2 μM.
体外活性
Tenatoprazole inhibits hog gastric H + /K + -ATPase activity with almost equal potency to that of omeprazole (IC 50 =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].
体内活性
Tenatoprazole inhibits basal gastric acid secretion in pylorus-ligated rats in a dose-dependent manner (ED 50 =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].
化学信息
分子量368.39
分子式C16H17N4NaO3S
CAS No.335299-59-7
储存&溶解度
存储Shipping with blue ice.

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  • 稀释 计算器
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TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

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