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Triamterene is a barosensitive epithelial sodium channel (ENaC) blocker with a diuretic effect. It can also act as an inhibitor of the TGR5 receptor, reducing GLP-1 secretion and cAMP level increases induced by TGR5 activation in a dose-dependent manner.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 50 mg | $29 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $29 | - | In Stock |
| Description | Triamterene is a barosensitive epithelial sodium channel (ENaC) blocker with a diuretic effect. It can also act as an inhibitor of the TGR5 receptor, reducing GLP-1 secretion and cAMP level increases induced by TGR5 activation in a dose-dependent manner. |
| Targets&IC50 | ENaC:4.5 μM, ENaCαS583:23.9 μM |
| In vitro | Triamterene's 4'-hydroxylation in the human body appears to be mediated solely by CYP1A2. The inhibition or induction of CYP1A2 can alter the temporal profile of both Triamterene and its active phase II metabolites. |
| In vivo | Triamterene inhibits epithelial sodium channels in the distal convoluted tubule and collecting duct principal cells, leading to a reduction in total sodium reabsorption by 1-2%. By impeding sodium reabsorption, triamterene also diminishes potassium secretion. Normally, potassium secretion is driven by the electrochemical gradient produced by sodium reabsorption. As sodium is reabsorbed, a negative potential is left in the tubular lumen while a positive potential is created in the principal cells. This electrical potential promotes potassium excretion through apical potassium channels. |
| Synonyms | SKF8542, Ademine |
| Molecular Weight | 253.26 |
| Formula | C12H11N7 |
| Cas No. | 396-01-0 |
| Smiles | Nc1nc(N)c2nc(c(N)nc2n1)-c1ccccc1 |
| Relative Density. | 1.502 g/cm3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| Solubility Information | DMSO: 3.33 mg/mL (13.15 mM), Sonication is recommended. Ethanol: < 1 mg/mL (insoluble or slightly soluble) H2O: < 1 mg/mL (insoluble or slightly soluble) | ||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (3.95 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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