Triamterene,396-01-0

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产品名称：Triamterene

产品别名：氨苯蝶啶

英文别名：Ademine

靶点：ENaC ，ENaCαS583

CAS：396-01-0

纯度：>98%

外观：黄色结晶性粉末

保存方法：-20°C

描述：

Triamterene blocks epithelial Na+ channel (ENaC) in a voltage-dependent manner with IC50 of 4.5 μM.

溶解性：DMSO ：16 mg/mL (63.2 mM)

体外研究：

Triamterene inhibits the epithelial sodium channels on principal cells in the late distal convoluted tubule and collecting tubule, which are responsible for 1-2% of total sodium reabsorption. Triamterene can achieve a modest amount of diuresis by decreasing the osmotic gradient necessary for water reabsorption from lumen to interstitium. Triamterene also has a potassium-sparing effect. Normally, the process of potassium excretion is driven by the electrochemical gradient produced by sodium reabsorption. As sodium is reabsorbed, it leaves a negative potential in the lumen, while producing a positive potential in the principal cell. This potential promotes potassium excretion through apical potassium channels. By inhibiting sodium reabsorption, triamterene also inhibits potassium excretion.

体内研究：4'-hydroxylation of triamterene in humans appears to be mediated exclusively by CYP1A2. Inhibition or induction of CYP1A2 will change the time course of both triamterene and its active phase-II metabolite.

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