Istaroxime
Catalog No.
A3507
Na+/K+ ATPase的抑制剂
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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
- 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
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-cyclopenta[a]phenanthrene-6,17(10H,14H)-dione |
SDF | Download SDF |
Canonical SMILES | CC12CC/C(CC1C(CC3C2CCC4(C)C3CCC4=O)=O)=N\OCCN |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |