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
- 화학식: C24H39NO4
- 분자량:405.58
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
제품 설명
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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분자량 405.58
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)