Chemical Structure : Istaroxime hydrochloride
CAS No.: 374559-48-5
Catalog No.: PC-49732Not For Human Use, Lab Use Only.
Istaroxime (PST2744) is an inotropic agent and Na(+)/K(+)-ATPase inhibitor, inhibits dog kidney Na(+)/K(+)-ATPase with IC50 of 0.43 uM, also stimulates SERCA2a.
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Istaroxime (PST2744) hydrochloride is an inotropic agent and Na(+)/K(+)-ATPase inhibitor, inhibits dog kidney Na(+)/K(+)-ATPase with IC50 of 0.43 uM, also stimulates SERCA2a.
Istaroxime (0.2 mg/kg/min) exerted an immediate and long-lasting inotropic effect (ED(80) of 1.89 mg/kg) without causing lethal arrhythmias in in anesthetized guinea pigs.
Istaroxime significantly increased resting values of +dP/dt(max), left ventricular pressure, and SPB, and increased +dP/dt(max) throughout treadmill exercise in conscious dogs with a healed myocardial infarction.
Istaroxime (100 nmol/L) normalized the depressed (-32%) SERCA2a maximum velocity and increased SERCA activity (+17%) in left ventricular sarcoplasmic reticulum microsomes from AoB animals.
Istaroxime stimulates SERCA2a and accelerates calcium cycling in heart failure by relieving phospholamban inhibition. Istaroxime combines Na+-K+-ATPase (NKA) inhibition with sarco/endoplasmic reticulum Ca2+-ATPase 2a (SERCA2a) stimulation.
M.Wt | 396.96 | |
Formula | C21H33ClN2O3 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
[E,Z]-3-[(2-aminoethoxy)imino]-androstane-6,17-dione hydrochloride |
1. Micheletti R, et al. Am J Cardiol. 2007 Jan 22;99(2A):24A-32A.
2. Ferrandi M, et al. Br J Pharmacol. 2013 Aug;169(8):1849-61.
3. Wallner M, et al. Oncotarget. 2017 Jul 25;8(30):49264-49274.
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