Istaroxime
Based on 7 publication(s) in Google Scholar
Istaroxime (PST2744) is a potent inhibitor of Na+,K+-ATPase with IC50 of 0.11 μM.
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- CAS No.: 203737-93-3
- Formule: C21H32N2O3
- Masse moléculaire:360.49
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Istaroxime
More- Ann Rheum Dis. 2022 Apr;81(4):544-555. [Abstract]
- 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]
Activité biologique
Description
IC50 & Target
IC50: 0.11 μM (Na+,K+-ATPase)[1]
In Vitro
Istaroxime 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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 203737-93-3
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Masse moléculaire 360.49
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Formule C21H32N2O3
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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
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Synonyms
PST2744
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (7)
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Journal Impact Factor
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Most Recent
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Ann Rheum Dis
Digoxin targets low density lipoprotein receptor-related protein 4 and protects against osteoarthritis. [Abstract]2022 Apr;81(4):544-555. PMID: 34853001 -
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
Pureté et documentation
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Istaroxime Related Classifications
HY-15718 Related Classifications
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