Triamterene

Catalog No.S4080 Synonyms: SKF8542

Triamterene Chemical Structure

Molecular Weight(MW): 253.26

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

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In DMSO USD 130 In stock
USD 97 In stock
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Biological Activity

Description Triamterene blocks epithelial Na+ channel (ENaC) in a voltage-dependent manner with IC50 of 4.5 μM.
Targets
ENaC [1] ENaCαS583 [1]
4.5 μM 23.9 μM
In vitro

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. [2]

In vivo 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.[3]

Protocol

Solubility (25°C)

In vitro DMSO 20 mg/mL (78.97 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order:
0.5% CMC Na+1% Tween 80
30mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 253.26
Formula

C12H11N7

CAS No. 396-01-0
Storage powder
Synonyms SKF8542

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02522650 Recruiting Proteinuria Georgetown University July 2013 Phase 4
NCT00000525 Completed Cardiovascular Diseases|Death, Sudden, Cardiac|Heart Arrest|Heart Diseases|Hypertension University of California, San Francisco|National Heart, Lung, and Blood Institute (NHLBI) July 1986 Phase 3

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID