| Bioactivity | Istaroxime hydrochloride is a Na+/K+-ATPase inhibitor (IC50=0.11 μM) and a sarcoplasmic/endoplasmic reticulum calcium ATPase 2 (SERCA 2) activator. |
| Target | IC50: 0.11 μM (Na+,K+-ATPase) |
| Invitro | Istaroxime hydrochloride 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/dtmax 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 (EDmax) of 4.88±0.6 mg/kg[3]. |
| Name | Istaroxime hydrochloride |
| CAS | 374559-48-5 |
| Formula | C21H33ClN2O3 |
| Molar Mass | 396.95 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. Gobbini M, et al. Novel analogues of istaroxime, a potent inhibitor of Na+,K+-ATPase: synthesis and structure-activity relationship. J Med Chem. 2008 Aug 14;51(15):4601-8. [2]. Gobbini M, et al. Novel analogues of Istaroxime, a potent inhibitor of Na(+),K(+)-ATPase: Synthesis, structure-activity relationship and 3D-quantitative structure-activity relationship of derivatives at position 6 on the androstane scaffold. Bioorg Med Ch [3]. Micheletti R, et al. Pharmacological profile of the novel inotropic agent (E,Z)-3-((2-aminoethoxy)imino)androstane-6,17-dione hydrochloride (PST2744). J Pharmacol Exp Ther. 2002 Nov;303(2):592-600. |