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Amiloride is a potassium-sparing diuretic.1,2 It is an inhibitor of the epithelial sodium channel (ENaC; K0.5 = 2.6 µM for recombinant δENaC expressed in X. laevis oocytes).3 It inhibits sodium transport from bovine kidney cortex membrane vesicles with an IC50 value of 0.4 µM.4 Amiloride inhibits the urokinase-type plasminogen activator (u-PA; Ki = 7 µM) and cardiac Na+/H+-ATPase (IC50 = 83.8 µM).5,6 It also inhibits calcium currents mediated by transient receptor potential polycystin 3 (TRPP3; IC50 = 143 µM).7 Amiloride (30 mg/kg) reduces mean arterial pressure in spontaneously hypertensive, but not normotensive, rats.8 Formulations containing amiloride have been used alone, and in combination with thiazide diuretics, in the treatment of hypertension.
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1. Physiological society symposium: Ion channels in health and disease. Molecular biology of the amiloride-
2. ENaCs and ASICs as therapeutic targets. Am. J. Physiol. Cell Physiol. 302(7), C943-C965 (2012).
3. Molecular cloning and functional expression of a novel amiloride-
4. Photoaffinity labeling of the epithelial sodium channel. The Journal of Biological Chemisty 261(6), 2839-2843 (1986).
5. Amiloride selectively inhibits the urokinase-
6. Amiloride and its analogs as tools in the study of ion transport. J. Membr. Biol. 105(1), 1-21 (1988).
7. Inhibition of TRPP3 channel by amiloride and analogs. Mol. Pharmacol. 72(6), 1576-1585 (2007).
8. Myocardial and vascular actions of amiloride in spontaneously hypertensive rats. J. Pharmacol. Exp. Ther. 239(2), 365-374 (1986).