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156722-18-8 (Rostafuroxin)

1

Identification

Rostafuroxin Rostafuroxin
Name Rostafuroxin
Formula C23H34O4
MW 374.51
CAS No. 156722-18-8
EINECS
Smiles O[[email protected]]([[email protected]@](CC[[email protected]@]1([H])[[email protected]@]2(CC[[email protected]](O)C1)C)([H])[[email protected]]2([H])CC3)(CC[[email protected]@]4(C5=COC=C5)O)[[email protected]]34C
Synonyms PST-2238;PST 2238;PST2238; (3S,5R,8R,9S,10S,13S,14S,17S)-17-(furan-3-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthrene-3,14,17-triol
InChI InChI=1S/C23H34O4/c1-20-8-5-17(24)13-15(20)3-4-19-18(20)6-9-21(2)22(25,10-11-23(19,21)26)16-7-12-27-14-16/h7,12,14-15,17-19,24-26H,3-6,8-11,13H2,1-2H3/t15-,17+,18+,19-,20+,21-,22+,23+/m1/s1
2

Introduction

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.

Background Information

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 ......by ProbeChem
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.
3

Protocol(Only for Reference)

Cell Experiment

Animal Experiment

4

Physical and Chemical Properties

Appearance:White to off-white Solid EBNumber:EB000010081

Storage condition

4°C by MedChemexpress Co., Ltd.

Solubility

100 mM in DMSO by CHEMSCENE, LLC
100 mM in DMSO by MedChemexpress Co., Ltd.
5

Mechanism and Indication

6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
Rostafuroxin sigma-tau i.f.r. S.p.A. Essential Hypertension 2006/12/21 Phase 2 Clinical
Rostafuroxin - Phase 2
7

Safety Data of Rostafuroxin

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Spectral Information

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Suppliers List

Company Price and Availability Country/Region
AOBIOUS INC 1mg/USD17();5mg/USD72() USA
AbMole BioScience 5mg/USD90(In stock) USA
AdooQ BioScience, LLC 5mg/USD96() USA
Apexbio Technology LLC USA
Ark Pharm, Inc. USA
BOC Sciences
Biochempartner Co., Ltd China
CHEMSCENE, LLC 10mg/USD162();50mg/USD702() USA
Cayman Chemical Company USA
DC Chemicals 100mg/USD550(In stock) China
Lancrix Chemicals. 25mg/USD230() China
MedChemexpress Co., Ltd. 10mg/USD162();50mg/USD702() USA
MedKoo Biosciences, Inc. USA
ProbeChem
Shanghai Haoyuan Chemexpress Co., Ltd. 10mg/USD162();50mg/USD702() China
Target Molecule Corp. 1mg/USD42();5mg/USD102();10mg/USD158();25mg/USD285();50mg/USD525() USA
Tocris Bioscience Inc. 10mg/USD185() USA
10

Related Products

Other Forms of 156722-18-8

Name CAS No Formula MW

Recommended Compounds in Na+/K+ ATPase

Name CAS No Formula MW
Ouabain (Octahydrate) 11018-89-6 C29H44O12 584.65
Prilocaine (hydrochloride) 1786-81-8 C13H21ClN2O 256.77
Prilocaine 721-50-6 C13H20N2O 220.31
Istaroxime (hydrochloride) 374559-48-5 C21H33ClN2O3 396.95
Istaroxime 203737-93-3 C21H32N2O3 360.49
Digitoxin 71-63-6 C41H64O13 764.94
Chlorpropamide 94-20-2 C10H13ClN2O3S 276.7398
Digoxin 20830-75-5 C41H64O14 780.94
Suloctidil 54767-75-8 C20H35NOS 337.56
Ouabain (Octahydrate) 11018-89-6 C29H60O20 728.77

Recommended Compounds in Same Indication

Name CAS No Formula MW
Azilsartan (medoxomil) 863031-21-4 C30H24N4O8 568.53
Azilsartan 147403-03-0 C25H20N4O5 456.45
AHU-377 (hemicalcium salt) 1369773-39-6 C24H28NO5- 410.48
LCZ696 936623-90-4 C48H55N6Na3O8 912.96
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Route of Synthesis

12

References

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More Information

Rostafuroxin

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