Tenatoprazole sodium
(Synonyms: 泰妥拉唑钠,TU-199 sodium) 目录号 : GC37756
A proton pump inhibitor
Cas No.:335299-59-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Tenatoprazole is a proton pump inhibitor, blocking hog gastric H+/K+-ATPase activity with an IC50 value of 6.2 ?M.1 It is orally bioavailable, blocking induced gastric acid secretion and ulcer formation in rats and humans.1,2,3 Tenatoprazole has a prolonged plasma half-life resulting in persistent effectiveness after withdrawal.3
1.Uchiyama, K., Wakatsuki, D., Kakinoki, B., et al.Effects of TU-199, a novel H+, K(+)-ATPase inhibitor, on gastric acid secretion and gastroduodenal ulcers in ratsMethods Find. Exp. Clin. Pharmacol.21(2)115-122(1999) 2.Galmiche, J.P., Bruley Des Varannes, S., Ducrotté, P., et al.Tenatoprazole, a novel proton pump inhibitor with a prolonged plasma half-life: effects on intragastric pH and comparison with esomeprazole in healthy volunteers.Aliment Pharmacol. Ther.19(6)655-662(2004) 3.Hunt, R.H., Armstrong, D., James, C., et al.Effect on intragastric pH of a PPI with a prolonged plasma half-life: Comparison between tenatoprazole and esomeprazole on the duration of acid suppression in healthy male volunteersAm. J. Gastroenterol.100(9)1949-1956(2005)
| Cas No. | 335299-59-7 | SDF | |
| 别名 | 泰妥拉唑钠,TU-199 sodium | ||
| Canonical SMILES | CC(C(OC)=C(C)C=N1)=C1CS(C2=NC3=NC(OC)=CC=C3N2)=O.[Na] | ||
| 分子式 | C16H18N4NaO3S | 分子量 | 369.39 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7072 mL | 13.5358 mL | 27.0717 mL |
| 5 mM | 0.5414 mL | 2.7072 mL | 5.4143 mL |
| 10 mM | 0.2707 mL | 1.3536 mL | 2.7072 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
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.PMID:16405921DOI:10.1016/j.bcp.2005.11.030.
Tenatoprazole is a prodrug of the proton pump inhibitor (PPI) class, which 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(-1) of the enzyme in vitro. In vivo, maximum binding of Tenatoprazole was 2.9 nmol mg(-1) of the enzyme at 2 h after IV administration. The binding sites of Tenatoprazole were in the TM5/6 region at Cys813 and Cys822 as shown by tryptic and thermolysin digestion of the ATPase labeled by Tenatoprazole. Decay of Tenatoprazole binding on the gastric H+,K+ -ATPase consisted of two components. One was relatively fast, with a half-life 3.9 h due to reversal of binding at cysteine 813, and the other was a plateau phase corresponding to ATPase turnover reflecting binding at cysteine 822 that also results in sustained inhibition in the presence of reducing agents in vitro. The stability of inhibition and the long plasma half-life of Tenatoprazole should result in prolonged inhibition of acid secretion as compared to omeprazole. Further, the bioavailability of Tenatoprazole was two-fold greater in the (S)-tenatoprazole sodium salt hydrate form as compared to the free form in dogs which is due to differences in the crystal structure and hydrophobic nature of the two forms.