Istaroxime(PST2744)

  Cat. No.:  DC7151  
Chemical Structure
203737-93-3
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Field of application
Istaroxime(PST2744) is a positive inotropic agent that mediates its action through inhibition of sodium/potassium adenosine triphosphatase (Na+/K+ ATPase).
Cas No.: 203737-93-3
Chemical Name: (3E,5S,8R,9S,10R,13S,14S)-3-(2-aminoethoxyimino)-10,13-dimethyl-1,2,4,5,7,8,9,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthrene-6,17-dione
Synonyms: PST-2744; PST 2744; PST2744
SMILES: O=C1CC[C@@]2([H])[C@]3([H])CC([C@@]4([H])C/C(CC[C@]4(C)[C@@]3([H])CC[C@@]21C)=N/OCCN)=O
Formula: C21H32N2O3
M.Wt: 360.49
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: IC50 Value: 0.43 ± 0.15 μM (Na+/K+-ATPase activity from dog kidney)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 . 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 . 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 . 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%) . 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) . 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 2For the detailed information of Istaroxime(PST2744), the solubility of Istaroxime(PST2744) in water, the solubility of Istaroxime(PST2744) in DMSO, the solubility of Istaroxime(PST2744) in PBS buffer, the animal experiment (test) of Istaroxime(PST2744), the cell expriment (test) of Istaroxime(PST2744), the in vivo, in vitro and clinical trial test of Istaroxime(PST2744), the EC50, IC50,and Affinity of Istaroxime(PST2744), Please contact DC Chemicals.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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