istaroxime hydrochloride

Istaroxime hydrochloride (PST2744 hydrochloride) is a Na+/K+-ATPase inhibitor and sarcoplasmic/endoplasmic reticulum calcium ATPase 2 (SERCA 2) activator, a novel positive inotropic compound that can be used to study acute heart failure.

Istaroxime, also known as PST-2744, is a positive inotropic agent that mediates its action through inhibition of sodium/potassium adenosine triphosphatase (Na+/K+ ATPase). Na+/K+ ATPase inhibition increases intracellular sodium levels, which reverses the driving force of the sodium/calcium exchanger, inhibiting calcium extrusion and possibly facilitating calcium entry. Additionally, Istaroxime increases intracellular calcium by improving the efficacy by which intracellular calcium triggers sarcoplasmic reticulum calcium release, and by accelerating the inactivation state of L-type calcium channels, which allow for calcium influx.

Istaroxime is an effective inhibitor of Na+, K+-ATPase (IC50: 0.11 μM).