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Ouabain Octahydrate

CAS No. : 11018-89-6

產品活性：Ouabain Octahydrate is an inhibitor of Na⁺/K⁺-ATPase, used for the treatment of congestive heart failure.

研究領域：Membrane Transporter/Ion Channel  |  Autophagy

作用靶點：Na+/K+ ATPase  |  Autophagy

結構分類：甾體類

In Vitro: Ouabain (100 μM) induces NLRP3 inflammasome activation and IL-1β release in macrophages. Ouabain-induced NLRP3 inflammasome activation is mediated through K⁺ efflux. Ouabain (3 nM) alters the expression of EMT markers in NHK and ADPKD cells, and modifies cell-cell adhesion properties in ADPKD. Moreover, ouabain enhances migration of ADPKD cells, selectively modulates tight junctions, and modulates adherens junctions in ADPKD cells in a selective manner. Ouabain also activates TGFβ-Smad3 signaling, alters TER in ADPKD cells. Ouabain (25, 50 or 100 nM) treatment significantly reduces cell proliferation and viability in Raji cells in a dose-dependent manner, with IC₅₀ of 76.48±4.03 nM. Ouabain increases the number of apoptotic cells, induces autophagy, and upregulates Beclin-1 in Raji cells.

In Vivo: Ouabain (3 mg/kg) significantly decreases cardiac contractile force with an enlarged LVESD when mice are primed with LPS. IL-1β deficiency attenuates ouabain-induced cardiac dysfunction and injury. IL-1β secreted by infiltrated macrophages contributes to ouabain-induced cardiac inflammation. Deficiency of NLRP3 and Casp1 attenuates ouabain-induced cardiac dysfunction and macrophage infiltration. Ouabain (30 µg/kg, i.p.) modulates ABCB1 activity in thymocytes of Wistar rats and it has the same effect on Swiss mice at 300 µg/kg. After 14 days of ouabain treatment, the MAP of rats is significantly elevated.

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