Tenatoprazolesodium - CAS:335299-59-7 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	Tenatoprazolesodium
英文名称:	Tenatoprazolesodium
别名:	泰妥拉唑钠 Tenatoprazolesodiumsalt
CAS No:	335299-59-7	分子式:	C₁₆H₁₈N₄NaO₃S	分子量:	369.39
CAS No:	335299-59-7
分子式:	C₁₆H₁₈N₄NaO₃S
分子量:	369.39

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T11142 Tenatoprazolesodium (psaitong)

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包装规格：

5mg in glass bottle

产品描述：

基本信息

产品编号：	T11142
产品名称：	Tenatoprazolesodium
CAS:	335299-59-7	储存条件	粉末	-20℃	四年
分子式：	C16H18N4NaO3S		溶于液体	-80℃	一年
分子量：	369.39
化学名：	Tenatoprazole sodium salt
Solubility (25°C)：
体外:	DMSO
	Ethanol
	Water
体内(现配现用):
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
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。

生物活性

产品描述	一种质子泵抑制剂;抑制猪胃H+/K+-ATPase酶活性的IC50值为6.2μM。
靶点	IC50:6.2μM (H+/K+-ATPase)
体外研究	Tenatoprazole inhibits hog gastric H+/K+-ATPase activity with almost equal potency to that of omeprazole (IC50=6.2 and 4.2 microM,respectively).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 2.6nmol/mg of the enzyme.
体内研究	Tenatoprazole inhibits basal gastric acid secretion in pylorus-ligated rats in a dose-dependent manner (ED50=4.2mg/kg p.o.).In gastric fistula rats, tenatoprazole (2.5 and 5mg/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.Maximum binding of tenatoprazole is 2.9nmol/mg of the enzyme at 2h 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.

推荐实验方法(仅供参考)

激酶实验：

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

动物实验:

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

保存条件：

-20℃

UN码：

HazardClass：

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安全说明：

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