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> Istaroxime (hydrochloride) [374559-48-5]

Istaroxime (hydrochloride) [374559-48-5]

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Cat# HY-15718A-50mg

Size : 50mg

Brand : MedChemExpress


Istaroxime hydrochloride is a Na+/K+-ATPase inhibitor (IC50=0.11 μM) and a sarcoplasmic/endoplasmic reticulum calcium ATPase 2 (SERCA 2) activator.

For research use only. We do not sell to patients.

Istaroxime hydrochloride Chemical Structure

Istaroxime hydrochloride Chemical Structure

CAS No. : 374559-48-5

This product is a controlled substance and not for sale in your territory.

Based on 5 publication(s) in Google Scholar

Other Forms of Istaroxime hydrochloride:

  • Istaroxime Get quote
  • Istaroxime oxalate Get quote

View All Calcium Channel Isoform Specific Products:

View All Isoforms
N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel
Description

Istaroxime hydrochloride is a Na+/K+-ATPase inhibitor (IC50=0.11 μM) and a sarcoplasmic/endoplasmic reticulum calcium ATPase 2 (SERCA 2) activator.

IC50 & Target

IC50: 0.11 μM (Na+,K+-ATPase)[1]
In Vitro

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.

Istaroxime hydrochloride Related Antibodies
In Vivo

Istaroxime (PST2744) induces a progressive increase in +dP/dtmax throughout the infusion that reaches 80% (ED80) at the cumulative dose of 1.89±0.37 mg/kg and a peak of 140±3.5% at the dose (EDmax) of 4.88±0.6 mg/kg[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

396.95

Formula

C21H33ClN2O3
CAS No.

374559-48-5
Appearance

Solid

Color

White to light brown

SMILES

O=C1CC[C@@]2(03)[C@]3(03)CC([C@@]4(03)C/C(CC[C@]4(C)[C@@]3(03)CC[C@@]21C)=N/OCCN)=O.03Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5192 mL 12.5960 mL 25.1920 mL
5 mM 0.5038 mL 2.5192 mL 5.0384 mL
View the 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.

* 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.

  • Protocol 1

    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

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.32%

COA (249 KB) HNMR (186 KB) LCMS (237 KB)

Handling Instructions (2659 KB)
References

  • [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]

Kinase Assay
[3]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[3]

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

  • [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]

  • [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.

    [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

    [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.

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.

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Istaroxime hydrochloride Related Classifications

  • Membrane Transporter/Ion Channel Neuronal Signaling
  • Na+/K+ ATPase Calcium Channel
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Keywords:

Istaroxime374559-48-5PST2744PST 2744PST-2744Na+/K+ ATPaseCalcium ChannelSodium potassium pumpCa2+ channelsCa channelsInhibitorinhibitorinhibit

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HY-15718A-100mg
Istaroxime (hydrochloride) [374559-48-5]
 100mg