Amiloride

• CAT Number: I002891
• CAS Number: 2609-46-3
• Molecular Formula: C6H8ClN7O
• Molecular Weight: 229.63
• Purity: ≥95%
• Target: Sodium Channel
• Solubility: 10 mM in DMSO
• Storage: Store at -20 C

Amiloride is a potent epithelial sodium channel blocker.Target: Sodium ChannelAmiloride is a pyrazine compound inhibiting sodium reabsorption through sodium channels in renal epithelial cells. This inhibition creates a negative potential in the luminal membranes of principal cells, located in the distal convoluted tubule and collecting duct. Negative potential reduces secretion of potassium and hydrogen ions. Amiloride is used in conjunction with diuretics to spare potassium loss. Amiloride works by directly blocking the epithelial sodium channel (ENaC) thereby inhibiting sodium reabsorption in the late distal convoluted tubules, connecting tubules, and collecting ducts in the kidneys. This promotes the loss of sodium and water from the body, but without depleting potassium [1].Amiloride, the first ENaC blocker to be applied to δβγ channels, has an IC50 of 2.6 μM. The Ki of amiloride for δβγ ENaC is 26-fold that of αβγ channels (0.1 μM for αβγ ENaC). The Ki of amiloride for δαβγ channels was 920 and 13.7 μM at 120 and +80 mV, respectively, which significantly differed from that of both αβγ and δβγ channels [2].

Reference

[1]. Loffing, J. and B. Kaissling, Sodium and calcium transport pathways along the mammalian distal nephron: from rabbit to human. Am J Physiol Renal Physiol, 2003. 284(4): p. F628-43.
[2]. Ji, H.L., et al., delta ENaC: a novel divergent amiloride-inhibitable sodium channel. Am J Physiol Lung Cell Mol Physiol, 2012. 303(12): p. L1013-26.