|Ouabain inhibitor, ameliorating endothelial dysfunction and oxidative stress
......by AOBIOUS INC
|Rostafuroxin (PST 2238) is a new oral antihypertensive agent able to selectively antagonize EO, adducin pressor, and molecular effects. It is endowed with high potency and efficacy in reducing blood pressure and preventing organ hypertrophy in animal models representative of both adducin and EO mechanisms.At molecular level, in the kidney, Rostafuroxin antagonizes EO triggering of the Src-epidermal growth factor receptor (EGFr)-dependent signaling pathway leading to renal Na+-K+ pump, and ERK tyrosine phosphorylation and activation.In the vasculature, it normalizes the increased myogenic tone caused by nanomolar ouabain. A very high safety ratio and an absence of interaction with other mechanisms involved in blood pressure regulation, together with initial evidence of high tolerability and efficacy in hypertensive patients, indicate Rostafuroxin as the first example of a new class of antihypertensive agents designed to antagonize adducin and EO-hypertensive mechanisms.
......by AbMole BioScience
| Rostafuroxin (PST-2238) is an ouabain-inhibitor counteracting specific forms of hypertension.
......by AdooQ BioScience, LLC
|Rostafuroxin, as a Na+/K+ ATPase modulator it treats hypertension by normalizing renal Na+/K+ ATPase pump function.
Na+,K+-ATPase: IC50= 1.5 nM
......by BOC Sciences
|Rostafuroxin, also known as PST-2238, is an ouabain antagonist. Rostafuroxin protects from podocyte injury and proteinuria induced by adducin genetic variants and ouabain. Rostafuroxin ameliorates endothelial dysfunction and oxidative stress in resistance arteries from deoxycorticosterone acetate-salt hypertensive rats: the role of Na+K+-ATPase/ cSRC pathway. Rostafuroxin corrects renal and vascular Na+-K+- ATPase alterations in ouabain and adducin-dependent hypertension.
......by MedKoo Biosciences, Inc.
|Rostafuroxin (PST2238) is potent, selective, orally active Na-K-ATPase inhibitor, displaces 3H ouabain from dog kidney Na+,K+-ATPase with IC50 of 1.5 nM; displays excellent selectivity over a panel of general and hormonal receptors, with exception of thromboxane A2 receptor (61% inhibition at 1 uM); abolishes ouabain-dependent increase in the Na-K pump rate in cultured renal cells, abolishes the increase in blood pressure and renal Na-K ATPase activity caused by ouabain in rats model of hypertension.HypertensionPhase 2 Clinical
|A novel antihypertensive agent, rostafuroxin (PST2238), has been selected and developed for its ability to correct the renal Na(+)-K(+) pump abnormalities sustained by the mutant adducin and EO-dependent mechanisms.
......by Target Molecule Corp.
|Na+/K+ ATPase modulator. Inhibits the Normalizes renal Na+/K+ ATPase pump function in mutant adducin- and endogenous ouabain-dependent forms of hypertension. Reduces blood pressure in Milan hypertensive rats. Controls mania-like behaviors in Myshkin mice having a Na+/K+ ATPase α3 subunit mutation. Antagonizes the effects of Ouabain (Cat.No. 1076) on myogenic tone and Ca2+ signaling in rat hippocampal neurons.
......by Tocris Bioscience Inc.