1. Membrane Transporter/Ion Channel
  2. Na+/K+ ATPase
  3. Istaroxime hydrochloride

Istaroxime hydrochloride (Synonyms: PST2744 (hydrochloride))

Cat. No.: HY-15718A Purity: 99.32%
Handling Instructions

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

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 306 In-stock
Estimated Time of Arrival: December 31
5 mg USD 278 In-stock
Estimated Time of Arrival: December 31
10 mg USD 426 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1008 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1680 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Other Forms of Istaroxime hydrochloride:

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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].

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].

Clinical Trial
Molecular Weight

396.95

Formula

C₂₁H₃₃ClN₂O₃

CAS No.

374559-48-5

SMILES

O=C1CC[[email protected]@]2([H])[[email protected]]3([H])CC([[email protected]@]4([H])C/C(CC[[email protected]]4(C)[[email protected]@]3([H])CC[[email protected]@]21C)=N/OCCN)=O.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 45 mg/mL (113.36 mM)

*"≥" 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 25.1921 mL
5 mM 0.5038 mL 2.5192 mL 5.0384 mL
10 mM 0.2519 mL 1.2596 mL 2.5192 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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

Purity: 99.32%

  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Istaroxime hydrochloride
Cat. No.:
HY-15718A
Quantity: