Istaroxime hydrochloride (Synonyms: PST2744 hydrochloride)

Name: Istaroxime hydrochloride
Brand: MedChemExpress
SKU: HY-15718A
Rating: 5.0 (5 reviews)

Cat. No.: HY-15718A Purity: 99.28%: FAQs
Data Sheet SDS COA Handling Instructions

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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

CAS No. : 374559-48-5

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 306	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 306	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 278	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 380	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 950	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1425	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 5 publication(s) in Google Scholar

Other Forms of Istaroxime hydrochloride:

Istaroxime Get quote
Istaroxime oxalate Get quote

5 Publications Citing Use of MCE Istaroxime hydrochloride

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

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].

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

In Vivo

Istaroxime (PST2744) induces a progressive increase in +dP/dt_max 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 (ED_max) 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([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

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
10 mM	0.2519 mL	1.2596 mL	2.5192 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.30 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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)

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%

Select Batch:

Data Sheet (280 KB) SDS (252 KB)

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]

Complete Stock Solution Preparation Table

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
DMSO	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

Cardiovascular Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

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

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Istaroxime hydrochloride (Synonyms: PST2744 hydrochloride)

Customer Review

Other Forms of Istaroxime hydrochloride:

Istaroxime hydrochloride Related Antibodies

5 Publications Citing Use of MCE Istaroxime hydrochloride

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Calcium Channel Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Istaroxime hydrochloride Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Istaroxime hydrochloride Related Classifications

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