Istaroxime(PST2744,PST-2744)|cas 203737-93-3

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

Cat. No.	Product name	Field of application
DC47250	Nonanal	Nonanal is a saturated fatty aldehyde with antidiarrhoeal activity.
DC47249	Piperitone	Piperitone is as a powerful repellent and antiappetent agent. Piperitone is very toxic to Cymbopogon schoenanthus (C. schoenanthus) adults, newly laid eggs and to neonate larvae. Insecticidal activity.
DC47247	Tyrosylleucine TFA	Tyrosylleucine (Tyr-Leu, YL) TFA, an orally active dipeptide, exhibits a potent antidepressant-like activity.
DC47243	Dehydroglyasperin C	Dehydroglyasperin C, a isoflavone, is a potent NAD(P)H:oxidoquinone reductase (NQO1) and phase 2 enzyme inducer. Dehydroglyasperin C has antioxidant, neuroprotective, cancer chemopreventive, and anti-inflammatory activities.
DC47227	(−)-Myrtenal	(−)-Myrtenal ((1R)-(−)-Myrtenal) is an orally active terpene with antitumour activity. (−)-Myrtenal ameliorates hyperglycemia by enhancing GLUT2 through Akt in the skeletal muscle and liver of diabetic rats.
DC47224	GPX4-IN-3	GPX4-IN-3 (26a) is a potent glutathione peroxidase 4 (GPX4) inhibitor as a selective ferroptosis inducer. GPX4-IN-3 (26a) exhibits 71.7% inhibition for GPX4 with 1 μM.
DC47179	Tyrosylleucine	Tyrosylleucine (Tyr-Leu, YL), an orally active dipeptide, exhibits a potent antidepressant-like activity.
DC47178	Mead acid	Mead acid (5,8,11-Eicosatrienoic acid), an unsaturated (Omega-9) fatty acid, is an indicator of essential fatty acid deficiency.
DC47140	Yadanzioside K	Yadanzioside K is a natural quassinoid glucoside found in Brucea amarissima.
DC47105	Complanatoside B	Complanatoside B is a P. chinense Fisch flavonoid with potential anti-inflammatory effects.