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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 | Availability | Quantity |
---|---|---|---|
50 mg | $37 | In Stock | |
1 mL x 10 mM (in DMSO) | $59 | 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. |
Alias | 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. | ||||||||||||||||||||
Solubility Information | DMSO: 3.33 mg/mL (13.16 mM), Sonication is recommended. Ethanol: < 1 mg/mL (insoluble or slightly soluble) H2O: < 1 mg/mL (insoluble or slightly soluble) | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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