Ouabain Octahydrate is an inhibitor of Na/K-ATPase, used for the treatment of congestive heart failure.
体外研究
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.
体内研究
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.
分子式
C29H44O12
分子量
728.77
CAS号
11018-89-6
中文名称
毒毛旋花苷G
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
溶解性数据
In Vitro:
DMSO : 250 mg/mL (343.04 mM; Need ultrasonic)
H2O : 10 mg/mL (13.72 mM; ultrasonic and warming and heat to 60°C)