Triamterene

SKU: orb2281211

Description

Triamterene is a pressure-sensitive ENaC blocker used as a diuretic agent. It also functions as a TGR5 receptor antagonist, inhibiting TGR5-mediated GLP-1 secretion and cAMP elevation. This small molecule is applied in research on hypertension, fluid balance, and metabolic pathways in both cellular and animal models.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 396-01-0
• MW: 253.26
• Purity: 99.49% (May vary between batches)
• Formula: C₁₂H₁₁N₇
• SMILES: Nc1nc(N)c2nc(c(N)nc2n1)-c1ccccc1
• Target: GPCR19,Sodium Channel
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (3.95 mM);DMSO:3.33 mg/mL (13.15 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  ENaC:4.5 μM|ENaCαS583:23.9 μM
• 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.
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• 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Ademine, G-protein coupled receptor 19, G protein-coupled Bile Acid Receptor 1, GPBAR1, GPCR19, ENaC, ENaCαS583, Inhibitor, inhibit, Na channels, Na+ channels, SodiumChannel, Sodium Channel, SKF8542, SKF-8542, SKF 8542, Triamterene, TGR5

Compound Identifiers

PubChem CID

5546