Cassaine  (Synonyms: Nervocidine)

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^[1][2].

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.

405.58

C₂₄H₃₉NO₄

468-76-8

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]

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Clarke RL, et al. The Structure of Cassaic Acid. J. Am. Chem. Soc. 1966 Dec 1;88(24):5865–5871.

  [2]. Tobin T, et al. Cassaine: mechanism of inhibition of Na+ +K+ -ATPase and relationship of this inhibition to cardiotonic actions. Eur J Pharmacol. 1975;32(02):133-145.