Istaroxime hydrochloride
Based on 6 publication(s) in Google Scholar
Istaroxime hydrochloride is a Na+/K+-ATPase inhibitor (IC50=0.11 μM) and a sarcoplasmic/endoplasmic reticulum calcium ATPase 2 (SERCA 2) activator.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.90%
- CAS. Nr.: 374559-48-5
- Formel: C21H33ClN2O3
- Molecular Weight:396.95
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Publications Citing Use of MedChemExpress (MCE) Istaroxime hydrochloride
More- Nat Commun. 2025 Aug 29;16(1):8074. [Abstract]
- Biochem Pharmacol. 2023 May:211:115516. [Abstract]
- Biochem Pharmacol. 2020 Oct:180:114122. [Abstract]
- J Am Heart Assoc. 2021 Jul 20;10(14):e018833. [Abstract]
- Front Pharmacol. 2020 Dec 14:11:606097. [Abstract]
- PNAS Nexus. 2023 Dec 22;3(1):pgad453. [Abstract]
Alle Calcium Channel Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
IC50: 0.11 μM (Na+,K+-ATPase)[1]
Istaroxime hydrochloride acting as a positive inotropic compound through the inhibition of the Na+,K+-ATPase[2]. Istaroxime (PST2744) inhibits the Na+/K+-ATPase activity from dog kidney with an IC50 value of 0.43 ± 0.15 μM. Inhibition of Na+/K+-ATPase activity in preparations from guinea pig kidney yielded potencies of 8.5 μM for PST2744[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 374559-48-5
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Appearance Solid
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Molecular Weight 396.95
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Formel C21H33ClN2O3
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Color White to light brown
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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.[H]Cl
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Synonyms
PST2744 hydrochloride
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
Publications (6)
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Journal Impact Factor
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Most Recent
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Nat Commun
NEXN protects against vascular calcification by promoting SERCA2 SUMOylation and stabilization. [Abstract]2025 Aug 29;16(1):8074. PMID: 40883305 -
Biochem Pharmacol
Periplocin targets low density lipoprotein receptor-related protein 4 to attenuate osteoclastogenesis and protect against osteoporosis. [Abstract]2023 May:211:115516. PMID: 36966936 -
Biochem Pharmacol
Natural cardenolides suppress coronaviral replication by downregulating JAK1 via a Na+/K+-ATPase independent proteolysis. [Abstract]2020 Oct:180:114122. PMID: 32592721 -
J Am Heart Assoc
2021 Jul 20;10(14):e018833. PMID: 34219467 -
Front Pharmacol
Inhibition of SARS-CoV-2 by Highly Potent Broad-Spectrum Anti-Coronaviral Tylophorine-Based Derivatives. [Abstract]2020 Dec 14:11:606097. PMID: 33519469 -
PNAS Nexus
Mechanisms for cardiac calcium pump activation by its substrate and a synthetic allosteric modulator using fluorescence lifetime imaging. [Abstract]2023 Dec 22;3(1):pgad453. PMID: 38222469
Lösungsmittel & Löslichkeit
DMSO : ≥ 45 mg/mL (113.36 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 25 mg/mL (62.98 mM; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.30 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.30 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 12.5 mg/mL (31.49 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protokoll
Dog or guinea pig kidney outer medulla is homogenized with a Polytron in 250 mM sucrose and 30 mM histidine, at pH 7.2. The homogenate is centrifuged at 6,000g for 15 min at 4°C and the supernatant at 48,000g for 30 min at 20°C with SDS and then layered onto a discontinuous sucrose density gradient (10, 15, and 29%) and centrifuged at 60,000 rpm for 115 min at 4°C. The pellet is resuspended in 25 mM imidazole and 1 mM EDTA, pH 7.5. Protein content is measured. Na+/K+-ATPase activity is measured after the release of 32P from [32P]ATP. Increasing concentrations of compounds are preincubated with purified enzyme for 10 min at 37°C in 120 μL of final volume of medium containing 140 mM NaCl, 3 mM MgCl2, 50 mM HEPES-Tris, and 3 mM ATP, pH 7.5. After preincubation, 10 μL of incubation solution containing 10 mM KCl and 20 nCi of [32P]ATP (0.5-3 Ci/mmol) is added, and the reaction is carried out for 15 min at 37°C before being stopped by acidification with 30% (v/v) perchloric acid. 32P is separated by centrifugation with activated charcoal and radioactivity measured by liquid scintillation counting. Inhibitory activity is expressed as percentage of control sample, carried out in the absence of standard compound. IC50 is calculated by weighed nonlinear regression curve fitting to the mass-action equilibrium[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pigs[3]
Male guinea Pigs (350-450 g) are used. Istaroxime (300 μg/kg) or Digoxin (75 μg/kg) are given by i.v. bolus 10 and 20 min before starting the exercise, respectively, and compared with vehicle. The following variables, HR, ECG, LVP, and aortic pressures, are recorded through a computerized acquisition system, which calculated the left ventricular rates of pressure changes. Data are analyzed from the real-time digitized recordings. Control values are obtained before compound administration.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Gobbini M, et al. Novel analogues of istaroxime, a potent inhibitor of Na+,K+-ATPase: synthesis and structure-activity relationship. J Med Chem. 2008 Aug 14;51(15):4601-8. [Content Brief]
[2]. Gobbini M, et al. Novel analogues of Istaroxime, a potent inhibitor of Na(+),K(+)-ATPase: Synthesis, structure-activity relationship and 3D-quantitative structure-activity relationship of derivatives at position 6 on the androstane scaffold. Bioorg Med Ch [Content Brief]
[3]. Micheletti R, et al. Pharmacological profile of the novel inotropic agent (E,Z)-3-((2-aminoethoxy)imino)androstane-6,17-dione hydrochloride (PST2744). J Pharmacol Exp Ther. 2002 Nov;303(2):592-600. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.5192 mL | 12.5960 mL | 25.1920 mL | 62.9800 mL |
| 5 mM | 0.5038 mL | 2.5192 mL | 5.0384 mL | 12.5960 mL | |
| 10 mM | 0.2519 mL | 1.2596 mL | 2.5192 mL | 6.2980 mL | |
| 15 mM | 0.1679 mL | 0.8397 mL | 1.6795 mL | 4.1987 mL | |
| 20 mM | 0.1260 mL | 0.6298 mL | 1.2596 mL | 3.1490 mL | |
| 25 mM | 0.1008 mL | 0.5038 mL | 1.0077 mL | 2.5192 mL | |
| 30 mM | 0.0840 mL | 0.4199 mL | 0.8397 mL | 2.0993 mL | |
| 40 mM | 0.0630 mL | 0.3149 mL | 0.6298 mL | 1.5745 mL | |
| 50 mM | 0.0504 mL | 0.2519 mL | 0.5038 mL | 1.2596 mL | |
| 60 mM | 0.0420 mL | 0.2099 mL | 0.4199 mL | 1.0497 mL | |
| DMSO | 80 mM | 0.0315 mL | 0.1575 mL | 0.3149 mL | 0.7873 mL |
| 100 mM | 0.0252 mL | 0.1260 mL | 0.2519 mL | 0.6298 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Istaroxime hydrochloride Related Classifications
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