tcsc1531 Istaroxime

Istaroxime is a potent inhibitor of Na⁺,K⁺-ATPase with IC₅₀ of 0.11 μM.







IC50 & Target: IC50: 0.11 μM (Na⁺,K⁺-ATPase)^[1]

In Vitro: Istaroxime acting as a positive inotropic compound through the inhibition of the Na⁺,K⁺-ATPase^[2]. Istaroxime (PST2744) inhibits the Na⁺/K⁺-ATPase activity from dog kidney with an IC₅₀ value of 0.43 ± 0.15 μM. Inhibition of Na⁺/K⁺-ATPase activity in preparations from guinea pig kidney yielded potencies of 8.5 μM for PST2744^[3].

In Vivo: Istaroxime (PST2744) induces a progressive increase in +dP/dt_max throughout the infusion that reaches 80% (ED₈₀) at the cumulative dose of 1.89±0.37 mg/kg and a peak of 140±3.5% at the dose (ED_max) of 4.88±0.6 mg/kg^[3].