- 中文名称:
- 化合物 Tenatoprazole sodium
- 英文名称:
- Tenatoprazole sodium
- CAS号:
- 335299-59-7
- 品牌:
- TargetMol
- 产地:
- 美国
- 保存条件:
- Shipping with blue ice.
- 产品类别:
- 抑制剂
- 货号:
- T61445
Product Introduction
Bioactivity
名称 | Tenatoprazole sodium |
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]. |
存储条件 | Shipping with blue ice. |
Tenatoprazole sodium|TargetMol
TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿,致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区,已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库,以及多种类型的生化试剂产品,包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等,此外,我们还建设有CADD(计算机辅助药物设计)研究中心、药理实验室、药化合成平台三大技术中心,全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持,我们将有效帮助您缩短研发周期,取得更成功的结果。
成立日期 |
(12年)
|
注册资本 |
566.265100万人民币 |
员工人数 |
100-500人 |
年营业额 |
¥ 1亿以上 |
经营模式 |
贸易,工厂,试剂,定制,服务 |
主营行业 |
天然产物,生化试剂,分子生物学,分子砌块,生物技术服务 |
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