GLPBio

Istaroxime hydrochloride

Catalog No.: GC17786Purity:>99.00%
COASDSData Sheet

Los productos son exclusivamente para uso en investigación. No aptos para uso humano. No vendemos a pacientes.

Istaroxime hydrochloride
Cas No.: 374559-48-5
10mM (in 1mL DMSO)In Stock
$178.00
1
2mgIn Stock
$86.00
1
5mgIn Stock
$162.00
1
10mgIn Stock
$261.00
1
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com

Citas (Citations)

Actualmente no hay citas disponibles para este producto. A continuación se muestran publicaciones seleccionadas que citan productos GlpBio.
  • Nature cover
    Nature
    641, 529–536 (2025)
  • Nature cover
    Nature
    628, 630–638 (2024)
  • Nature cover
    Nature
    632, 686–694 (2024)
  • Nature cover
    Nature
    618, 1017–1023 (2023)
  • Nature cover
    Nature
    610, 366–372 (2022)
  • Cell cover
    Cell
    187(9):2288-2304 (2024)
  • Cell cover
    Cell
    183(7):1867-1883 (2020)
  • Science cover
    Science
    388(6745) (2025)
  • Science cover
    Science
    387(6739) (2025)
  • Science cover
    Science
    387(6734) (2025)
  • Cell Research cover
    Cell Research
    35, 97–116 (2025)
  • Cell Research cover
    Cell Research
    34, 683–706 (2024)
  • Cell Research cover
    Cell Research
    33, 273–287 (2023)
  • Cell Research cover
    Cell Research
    33, 546–561 (2023)
  • Cell Research cover
    Cell Research
    33, 904–922 (2023)
  • Cell Research cover
    Cell Research
    31, 1291–1307 (2021)

Descripción (Description)

Istaroxime hydrochloride(PST2744) is a novel inhibitor of Na+/K+-ATPase with IC50 value of 0.43±0.15μM [1].

In vitro studies show that Istaroxime can inhibit the activity of Na+/K+-ATPase from dog kidney without significant interaction with other several receptors. It demonstrates the selectivity of Istaroxime. Ex vivo studies show the inotropic effect can be achieved up to 60% for Istaroxime. Istaroxime can also increase the force of contraction of guinea pig paced left atria in the range 0.3 to 30μM. In vivo assays prove Istaroxime is consistently safer than digoxin [1].

Istaroxime is a steroidal drug unrelated to cardiac glycosides that improves cellular calcium cycling. The inhibition of Na+/K+-ATPase induces cytosolic calcium accumulation during systole (inotropism). Clinical studies has been done with istaroxime in phase II. Istaroxime could be a promising alternative for patients with acute heart failure syndrome for whom the therapeutic options are currently limited [2].

References:
[1] R. Micheletti, G. G. Mattera, M. Rocchetti, A. Schiavone, M. F. Loi, A. Zaza, R. J. P. Gagnol, S. De Munari, P. Melloni, P. Carminati, G. Bianchi, and P. Ferrari. Pharmacological profile of the novel inotropic agent (e,z)-3-((2-aminoethoxy)imino)androstane-6,17-dione hydrochloride (PST2744). The journal of pharmacology and experimental therapeutics. 2002, 303 (2): 592-600.
[2] Suruchi Aditya, Aditya Rattan. Istaroxime: A rising star in acute heart failure. Journal of Pharmacology and Pharmacotherapeutics. 2012, 3(4): 353-355.

Protocolo (Protocol)

Cell experiment: [1]

Cell lines

Guinea pig ventricular myocytes

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

4 μM, 0.5 s

Applications

Resting Ca2+ was similarly increased by istaroxime (from 61.3 to 92.4 nM). Istaroxime increased [Ca]SR-tot by 47%. Istaroxime increased the amount of Ca2+ extruded by the Na+/Ca2+ exchanger (CaNCX) during caffeine-induced transients (+130). Istaroxime shortened the time elapsing between the start of the caffeine pulse and SR Ca2+ release.
Animal experiment: [2]

Animal models

Bio TO.2 hamsters and Bio F1B hamsters

Dosage form

Oral administration, 30 mg/5 mL/kg/day

Applications

Heart function of istaroxime-treated hamsters was comparable to that of healthy animals, and had a significantly higher LVSP and both positive and negative dP/dT when compared with that of vehicle-treated animals. Coronary flow rate in hearts isolated from istaroxime-treated hamsters was higher than that from vehicle-treated Bio TO.2 animals. Besides that, Bio TO.2 hamsters treated with istaroxime had both time and frequency domain indexes of HRV, i.e. standard deviation of R-R intervals, TP, LF and HF, augmented with respect to vehicle-treated animals. Moreover , the LF/HF ratio of istaroxime-treated animals was similar to that observed in Bio F1B hamsters.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Rocchetti M, Besana A, Mostacciuolo G, et al. Modulation of sarcoplasmic reticulum function by Na+/K+ pump inhibitors with different toxicity: digoxin and PST2744 [(E, Z)-3-((2-aminoethoxy) imino) androstane-6, 17-dione hydrochloride]. Journal of Pharmacology and Experimental Therapeutics, 2005, 313(1): 207-215.

[2] Giudice P L, Mattera G G, Gagnol J P, et al. Chronic istaroxime improves cardiac function and heart rate variability in cardiomyopathic hamsters. Cardiovascular drugs and therapy, 2011, 25(2): 133-138.

Documentos del producto (Product Documents)

Purity:>99.00%Appearance:A solid
COASDSData Sheet

Propiedades químicas (Chemical Properties)

N.º CAS
374559-48-5
Nombre químico
(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;hydrochloride
SMILES
CC12CCC(=NOCCN)CC1C(=O)CC3C2CCC4(C3CCC4=O)C.Cl
Fórmula molecular
C21H33ClN2O3
Peso molecular
396.95
Solubilidad
DMSO : ≥ 45 mg/mL (113.36 mM); H2O : 25 mg/mL (62.98 mM; Need ultrasonic)
Almacenamiento
4°C, sealed storage, away from moisture
Consejos generales
Seleccione un disolvente adecuado según los datos de solubilidad del producto. Una vez preparada, divida la solución madre en alícuotas para evitar ciclos repetidos de congelación y descongelación.
Utilice las soluciones madre en un plazo de 6 meses si se conservan a -80°C, o de 1 mes si se conservan a -20°C.
Para mejorar la solubilidad, caliente el tubo a 37°C y soníquelo durante un periodo adecuado.
Condiciones de envío
Las muestras de evaluación se envían con acumuladores de frío. Los demás tamaños se envían a temperatura ambiente o, previa solicitud, con acumuladores de frío.

Calculadoras (Calculators)Molaridad / Dilución / Peso molecular / Conversión de unidades / Formulación in vivo / Solubilidad

g/mol

Reviews

Review for Istaroxime hydrochloride

Rating: 5
  • 5 Star100%
  • 4 Star0%
  • 3 Star0%
  • 2 Star0%
  • 1 Star0%