amiloride

Amiloride hydrochloride (Amiloride HCl) is an effective sodium channel blocker of epithelial.

5-(N,N-Hexamethylene)-amiloride (5-HMA) is an amiloride derivative that inhibits TRPA1-mediated calcium signaling (IC50: 35 μM). It functions as an inhibitor of the Na+ H+ exchanger (NHE) with Ki values ranging from 0.013 to 2.4 μM for various NHE isoforms. Additionally, 5-HMA blocks ASIC3 channels by 51% at 20 μM.

Amiloride hydrochloride dihydrate (Amiloride HCl dihydrate) 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 hydrochloride dihydrate is used in conjunction with DIURETICS to spare POTASSIUM loss.

Dimethylamiloride is a specific inhibitor of antiporters [1].

6-Iodoamiloride is a potent inhibitor of acid-sensing ion channel 1 (ASIC1), exhibiting an IC50 value of 88 nM. It also effectively inhibits ASIC3-mediated currents in rat dorsal root ganglion neurons, with an IC50 of 230 nM [1].

LLC1, a derivative of amiloride, exhibits cytotoxicity against breast cancer cells, particularly those resistant to other treatments. The compound demonstrates varied IC50 values across several breast cancer cell lines, including 13 mM for MCF7, 12 mM for MCF7 MX-100, 25 mM for MCF7 TS, 26 mM for MCF7 TR-1, and 19 mM for MCF7 TR-5. LLC1 holds potential for research in cancer therapy.

Benzamil is an epithelial sodium channel (ENaC) blocker that inhibits sodium transport from (IC50 = 4 nM) and binds to (Kd = 5 nM) bovine kidney cortex membrane vesicles.

Phenamil is an irreversible inhibitor of amiloride-sensitive Na channels; derivative of amiloride, synergizing bone formation with BMP2 and inhibits BMP2 induced cyst-like bone formation.