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. Nr.: 203737-93-3
- Formel: C21H32N2O3
- Molecular Weight:360.49
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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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]
Biologische Aktivität
Beschreibung
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.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 203737-93-3
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Molecular Weight 360.49
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
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
Reinheit & Dokumentation
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]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Istaroxime Related Classifications
HY-15718 Related Classifications
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