Triamterene
Catalog No.S4080 Synonyms: SKF8542
Molecular Weight(MW): 253.26
Triamterene blocks epithelial Na+ channel (ENaC) in a voltage-dependent manner with IC50 of 4.5 μM.
Purity & Quality Control
Choose Selective Sodium Channel Inhibitors
Biological Activity
| Description | Triamterene blocks epithelial Na+ channel (ENaC) in a voltage-dependent manner with IC50 of 4.5 μM. | ||||
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| Targets |
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| 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] |
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| 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 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 |
Bio Calculators
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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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