product name Triamterene
Description: Triamterene (also known as SKF8542) is a weak diuretic with potassium sparing properties. It blocks Na+ channel (ENaC) in a voltage-dependent manner with IC50 of 4.5 μM. 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.
References: Mol Pharmacol. 2003 Oct;64(4):848-56; Int J Clin Pharmacol Ther. 2005 Jul;43(7):327-34.
253.26
Formula
C12H11N7
CAS No.
396-01-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 20 mg/mL (79 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
0.5% CMC Na+1% Tween 80: 30 mg/mL
Synonyms
SKF8542
other peoduct :
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
| Animal model | |
| Formulation & Dosage | |
| References | Mol Pharmacol. 2003 Oct;64(4):848-56; Int J Clin Pharmacol Ther. 2005 Jul;43(7):327-34. |
