2. Membrane Transporter/Ion Channel
  3. Proton Pump
  4. Tenatoprazole sodium

Tenatoprazole sodium  (Synonyms: TU-199 sodium)

目录号: HY-17421A
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摩尔计算器

Tenatoprazole sodium (TU-199 sodium) 是质子泵抑制剂; 抑制猪胃H+/K+-ATPase酶活性的 IC50 值为6.2 μM。

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Tenatoprazole sodium Chemical Structure

Tenatoprazole sodium Chemical Structure

CAS No. : 335299-59-7

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Tenatoprazole sodium 的其他形式现货产品:

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Tenatoprazole sodium 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

IC50 & Target

IC50: 6.2 μM (H+/K+-ATPase)[1]
体外研究
(In Vitro)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Tenatoprazole sodium 相关抗体:
体内研究
(In Vivo)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

368.39

Formula

C16H17N4NaO3S
CAS 号
中文名称

泰妥拉唑钠
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献
Kinase Assay
[2]

The enzyme suspension (20 mg/mL) is incubated at 37°C in a buffer composed of 5 mM Pipes/Tris (pH 6.95), 2 mM MgCl2, 150 mM KCl, 3 mg/mL of valinomycin, 1 mM acridine orange, in the presence of 0.1 mM glutathione, in a SPEX spectrofluorometer for 5 min. Inhibitor (20 mM), omeprazole or tenatoprazole, is added and fluorescence is measured by excitation at 490 nm and emission at 530 nm. After 60 s, ATP (2 mM) is added to initiate acridine orange uptake as a measure of intra-vesicular acidification[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Rats: (R,S)-Tenatoprazole free form (50 mg/kg) or (S)-tenatoprazole sodium salt hydrate (50 mg/kg) is orally administered to dogs and the plasma level of tenatoprazole is measured as a function of time course. Similarly, (S)-tenatoprazole free form (100 mg/kg) or (S)-tenatoprazole sodium salt hydrate (100 mg/kg) is orally administered to dogs and the plasma level of tenatoprazole is measured as a function of time[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

Tenatoprazole sodium 相关分类

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Keywords:

Tenatoprazole335299-59-7TU-199泰妥拉唑钠TU199TU 199Proton PumpInhibitorinhibitorinhibit

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