| Identification | Back Directory | [Name]
Istaroxime | [CAS]
203737-93-3 | [Synonyms]
PST2744
CS-1089
PST-2744
PST 2744
Debio0614
Istaroxime
Debio 0614
PST2744/PST-2744
Istaroxime(PST2744)
PST2744; PST 2744; ISTAROXIME; DEBIO 0614; DEBIO0614
Androstane-3,6,17-trione, 3-[O-(2-aminoethyl)oxime], (5α)-
(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 | [Molecular Formula]
C21H32N2O3 | [MOL File]
203737-93-3.mol | [Molecular Weight]
360.5 |
| Chemical Properties | Back Directory | [Boiling point ]
511.1±60.0 °C(Predicted) | [density ]
1.34±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in H2O | [form ]
Powder | [pka]
9.49±0.10(Predicted) |
| Hazard Information | Back Directory | [Biological Activity]
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]. | [IC 50]
0.43 ± 0.15 μm (na+/k+-atpase activity from dog kidney) [1] |
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| Company Name: |
SPIRO PHARMA
|
| Tel: |
|
| Website: |
www.spiropharma.com.cn |
| Company Name: |
Musechem
|
| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
| Company Name: |
Twochem Co.Ltd.
|
| Tel: |
021-58111628 15800915896 |
| Website: |
cn.twochem.com |
|