A3507-5mg | Istaroxime [203737-93-3] Clinisciences

Background

Description: IC50 Value: 0.43 ± 0.15 μM (Na+/K+-ATPase activity from dog kidney) [1] Istaroxime is a positive inotropic agent that mediates its action through inhibition of sodium/potassium adenosine triphosphatase (Na+/K+ ATPase). Istaroxime is an investigational drug originally patented and developed by the italian pharmaceutical company Sigma-Tau. Istaroxime is now under development for treatment of acute decompensated heart failure by CVie Therapeutics. in vitro: PST2744 inhibited the Na+/K+-ATPase activity from dog kidney with an IC50 value of 0.43 ± 0.15 μM [1]. The transient inward current (I(TI)) induced by a Ca(2+) transient in the presence of complete Na(+)/K(+) pump blockade was inhibited (-43%) by PST2744 but not by digoxin [2]. in vivo: Intravenous infusion of 0.2 mg/kg/min PST2744 in anesthetized guinea pigs exerted an immediate and long-lasting inotropic effect (ED(80) of 1.89 +/- 0.37 mg/kg) without causing lethal arrhythmias up to a cumulative dose of 18 mg/kg [1]. Istaroxime intravenous infusion (0.11 mg/kg per min) significantly increased both indices of contraction and relaxation (fractional shortening, +18+/-3.7%; aortic flow rate, +19+/-2.9%; peak myocardial systolic velocity, +36+/-7%; circumferential fiber shortening, +24+/-4.1%; peak atrial flow velocity, +69+/-8.6%; isovolumic relaxation time, +19+/-6.9%; and peak myocardial early diastolic velocity, +42+/-12%) [3]. In 5 animals, PST-2744 effects were compared with dobutamine. Heart rates, PR intervals and QT intervals were unchanged following PST-2744 administration. PST-2744 increased contractility (+dP/dt) by 56% from 1881 +/- 282 mm Hg/s to 2939 +/- 734 mm Hg/s (P < 0.01) [4]. Clinical trial: HORIZON-HF: A Phase II Trial to Assess Hemodynamic Effects of Istaroxime in Patients With Worsening HF and Reduced LV Systolic Function. Phase 2

Product Citation

1. Lin Tang, Xinxun Xiao, et al. "Induction of oocyte maturation and changes in the biochemical composition, physiology and molecular biology of oocytes during maturation and hydration in the orange-spotted grouper (Epinephelus coioides." aquaculture 4 December 2019. PII: S0044-8486(19)33325-3.
2. Bossu A, Kostense A, et al. "Istaroxime, a positive inotropic agent devoid of proarrhythmic properties in sensitive chronic atrioventricular block dogs." Pharmacol Res. 2018 Jul;133:132-140. PMID:29753687

Chemical Properties

Storage	Store at -20°C
M.Wt	360.49
Cas No.	203737-93-3
Formula	C₂₁H₃₂N₂O₃
Synonyms	PST-2744;PST 2744;PST2744
Solubility	Soluble in H2O
Chemical Name	(E)-3-((2-aminoethoxy)imino)-10,13-dimethyldodecahydro-1H-cyclopentapmphenanthrene-6,17(10H,14H)-dione
SDF	Download SDF
Canonical SMILES	CC12CC/C(CC1C(CC3C2CCC4(C)C3CCC4=O)=O)=N\OCCN
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.