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    Triamterene (SKF8542)
    Triamterene (SKF8542)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1668
    CAS #: 396-01-0 Purity ≥98%

    Description: Triamterene (formerly SKF-8542; SKF8542; BRN-0266723; Dyrenium; Diucelpin; Diurene) is a diuretic commonly used in combination with thiazide diuretics (e.g. hydrochlorothiazide/triamterene) for the treatment of high blood pressure or swelling. Triamterene has potassium sparing properties, and also blocks Na+ channel (ENaC) in a voltage-dependent manner with an IC50 of 4.5 μM. 

    References: Mol Pharmacol. 2003 Oct;64(4):848-56; Int J Clin Pharmacol Ther. 2005 Jul;43(7):327-34.

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    Molecular Weight (MW)253.26 
    FormulaC12H11N7 
    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
    SynonymsSKF-8542; BRN 0266723; SKF 8542; BRN0266723; SKF8542; BRN-0266723; Triamterene; Diucelpin; Diurene 


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    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.

    In Vivo4'-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. 
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    References

    Mol Pharmacol. 2003 Oct;64(4):848-56; Int J Clin Pharmacol Ther. 2005 Jul;43(7):327-34. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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