Cassaine
Cassaine (Nervocidine) is a Na+/K+-ATPase inhibitor. Cassaine stabilizes phosphorylated intermediates, slows spontaneous dephosphorylation and blocks potassium-stimulated dephosphorylation. Cassaine exhibits non-competitive inhibition with respect to K+, shows inhibition enhanced by Pi and antagonized by Na+. Cassaine induces positive inotropic effects in perfused hearts with faster inotropy offset. Cassaine can be used for research on cardiac arrhythmias.
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- CAS No.: 468-76-8
- Formule: C24H39NO4
- Masse moléculaire:405.58
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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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Activité biologique
Description
In Vitro
Cassaine (Compound 1) shows an ultraviolet absorption maximum at 224 mμ with ε = 18,000 and a specific optical rotation of -108 degrees[1].
Cassaine (10 nM-100 μM) inhibits rat brain Na+/K+-ATPase[2].
Cassaine (1-10 μM; 10 min) non-competitively inhibits K+-activated rat brain Na+/K+-ATPase, abolishes K+-induced substrate inhibition, and its inhibitory effects are overcome by high K+ concentrations in a qualitatively competitive manner[2].
Cassaine (1 mM) inhibits formation of the phosphorylated intermediate of rat brain Na+/K+-ATPase in the presence of Mg2+, with this inhibition facilitated by Pi and antagonized by Na+[2].
Cassaine (0.1 mM) slows spontaneous dephosphorylation of the phosphorylated intermediate of rat brain Na+/K+-ATPase but reduces its steady-state level by stabilizing a slowly resphosphorylating enzyme form[2].
Cassaine (0.1 mM) stabilizes the phosphorylated intermediate of rat brain Na+/K+-ATPase, rendering it resistant to dephosphorylation by both K+ and ADP[2].
Cassaine (100 nM-1 mM) concentration-dependently increases the steady-state level of the phosphorylated intermediate of rat brain Na+/K+-ATPase in the presence of K+[2].
Cassaine (10 nM-1 mM) inhibits dog, guinea pig, and rat heart Na+/K+-ATPase with species-dependent sensitivity (most sensitive in dog, least in rat)[2].
Cassaine (0.1 mM) dissociates from guinea pig heart Na+/K+-ATPase more rapidly than from dog heart Na+/K+-ATPase[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
Chemical Information
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CAS No. 468-76-8
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Masse moléculaire 405.58
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Formule C24H39NO4
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SMILES
C[C@@]12[C@](C(C)(C)[C@@H](O)CC1)(CC(=O)[C@@]3([C@@]2(CC/C(=C\C(OCCN(C)C)=O)/[C@@H]3C)[H])[H])[H]
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Synonyms
Nervocidine
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Structure Classification
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Initial Source
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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.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Cassaine Related Classifications
HY-165443 Related Classifications
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