amiloride

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

Amiloride (MK-870) is an inhibitor of the epithelial sodium channel (ENaC) and the urokinase-type plasminogen activator receptor (uPAR). It also acts as a blocker of the polycystin-2 (PC2; TRPP2) channel.

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.

Amiloride Hydrochloride (Standard) is the standard substance of Amiloride Hydrochloride, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. Amiloride hydrochloride (Amiloride HCl) is an effective sodium channel blocker of epithelial.

Dimethylamiloride hydrochloride selectively inhibits Na⁺/H⁺ exchangers located in cellular membranes, leading to intracellular H⁺ retention and a reduction in intracellular pH, Dimethylamiloride hydrochloride additionally blocks TRPA1 ion channels with an IC50 of 80 µM, making it a valuable pharmacological tool for studying ion transport, pH homeostasis, sensory signaling, and inflammatory pain mechanisms.

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].

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.

Benzamil hydrochloride is a specific and potent sodium channel (ENaC) blocker.

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.

Pyrazinoylguanidine (PZG) is an analogue of the potassium-sparing diuretic amiloride. It can reduce systolic and diastolic blood pressure in patients with primary hypertension and has a slight effect on reducing heart rate without altering serum concentrations of electrolytes such as sodium, potassium, or chloride. Pyrazinoylguanidine also alleviates hyperglycemia and hyperinsulinemia in type 2 diabetes patients, lowers triglycerides, cholesterol, and free fatty acids, and can reverse the hyperglycemia and hyperlipidemia induced by thiazide diuretics like hydrochlorothiazide. Additionally, it inhibits renal tubular reabsorption of urea, enhancing urea clearance and excretion, thus reducing serum urea concentration and its toxic accumulation.

Phenamil methanesulfonate is a potent analog of Amiloride that functions as a strong and less reversible epithelial sodium channel (ENaC) blocker with an IC50 of 400 nM, Phenamil methanesulfonate also acts as a competitive inhibitor of TRPP3 and suppressing TRPP3-mediated calcium transport with an IC50 of 140 nM in Ca2+ uptake assays. Phenamil methanesulfonate robustly activates BMP signaling to promote bone repair, supporting its use in cystic fibrosis lung disease, ion channel biology, and regenerative medicine research.

Phenamil is an inhibitor of epithelial sodium channels, which activates the osteomorphin protein signalling pathway to promote bone repair and induces significant fat formation.