Rostafuroxin | CAS#156722-18-8 | Ouabain Antagonist

MedKoo Cat#: 329458 | Name: Rostafuroxin

Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

Rostafuroxin

CAS#156722-18-8

Theoretical Analysis

MedKoo Cat#: 329458

Name: Rostafuroxin

CAS#: 156722-18-8

Chemical Formula: C23H34O4

Exact Mass: 374.2457

Molecular Weight: 374.52

Elemental Analysis: C, 73.76; H, 9.15; O, 17.09

Price and Availability

Size	Price	Availability
5mg	USD 150.00	Ready to ship
10mg	USD 250.00	Ready to ship
25mg	USD 550.00	Ready to ship

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Related CAS #

No Data

Synonym

PST-2238; PST 2238; PST2238; Rostafuroxin

IUPAC/Chemical Name

(3S,5R,8R,9S,10S,13S,14S,17S)-17-(furan-3-yl)-10,13-dimethylhexadecahydro-14H-cyclopenta[a]phenanthrene-3,14,17-triol

InChi Key

AEAPORIZZWBIEX-DTBDINHYSA-N

InChi Code

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

SMILES Code

C[C@@]12[C@](C3=COC=C3)(O)CC[C@]1(O)[C@]4([H])CC[C@]5([H])C[C@@H](O)CC[C@]5(C)[C@@]4([H])CC2

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot#A8T11K20

QC Data

View QC data: current batch, Lot#A8T11K20

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

Rostafuroxin (PST 2238), a digitoxigenin derivative, is a potent Na+,K+-ATPase (ATP1A1) antagonist.

In vitro activity:

TBD

In vivo activity:

In order to investigate whether high EO (endogenous ouabain) levels may directly contribute to worsen renal damage caused by ischemia-reperfusion maneuver, rats were subcutaneously infused with exogenous ouabain (30 µg/kg/day) (OHR (ouabain) rats) for eight weeks, while control rats received saline (control rats). After four weeks, OHR rats were divided into two groups receiving vehicle (group 2) or an oral treatment of 100 µg/kg/day rostafuroxin (group 4) for four weeks. Analogously, the control rats were allocated to two groups receiving vehicle (group 3) or 100 µg/kg/day rostafuroxin (group 5) for four weeks. At the end, all rats were subjected to renal ischemia and sacrificed after five days of reperfusion. In OHR rats, SBP significantly increased versus control rats (153.4 ± 6.8 mmHg, n = 7, vs. 111.7 ± 2.8 mmHg, n = 7, p < 0.01). Rostafuroxin reduced SBP in OHR (−20 mmHg, n = 7, p < 0.01), but not in controls (+5 mmHg, n = 7), as previously shown. Reference: Int J Mol Sci. 2016 Oct; 17(10): 1728. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5085759/

	Solvent	mg/mL	mM
Solubility
	DMSO	43.7	116.76
	Ethanol	37.5	100.00

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 374.52 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

TBD

In vitro protocol:

1. Villa L, Buono R, Ferrandi M, Molinari I, Benigni F, Bettiga A, Colciago G, Ikehata M, Messaggio E, Rastaldi MP, Montorsi F, Salonia A, Manunta P. Ouabain Contributes to Kidney Damage in a Rat Model of Renal Ischemia-Reperfusion Injury. Int J Mol Sci. 2016 Oct 14;17(10):1728. doi: 10.3390/ijms17101728. PMID: 27754425; PMCID: PMC5085759. 2. Song H, Karashima E, Hamlyn JM, Blaustein MP. Ouabain-digoxin antagonism in rat arteries and neurones. J Physiol. 2014 Mar 1;592(5):941-69. doi: 10.1113/jphysiol.2013.266866. Epub 2013 Dec 16. Erratum in: J Physiol. 2014 Nov 1;592(Pt 21):4803. PMID: 24344167; PMCID: PMC3948557.

In vivo protocol:

1: Villa L, Buono R, Ferrandi M, Molinari I, Benigni F, Bettiga A, Colciago G, Ikehata M, Messaggio E, Rastaldi MP, Montorsi F, Salonia A, Manunta P. Ouabain Contributes to Kidney Damage in a Rat Model of Renal Ischemia-Reperfusion Injury. Int J Mol Sci. 2016 Oct 14;17(10). pii: E1728. PubMed PMID: 27754425; PubMed Central PMCID: PMC5085759. 2: Manunta P, Ferrandi M, Cusi D, Ferrari P, Staessen J, Bianchi G. Personalized Therapy of Hypertension: the Past and the Future. Curr Hypertens Rep. 2016 Mar;18(3):24. doi: 10.1007/s11906-016-0632-y. Review. PubMed PMID: 26915067. 3: Ferrandi M, Molinari I, Rastaldi MP, Ferrari P, Bianchi G, Manunta P. Rostafuroxin protects from podocyte injury and proteinuria induced by adducin genetic variants and ouabain. J Pharmacol Exp Ther. 2014 Nov;351(2):278-87. doi: 10.1124/jpet.114.217133. PubMed PMID: 25187430. 4: Song H, Karashima E, Hamlyn JM, Blaustein MP. Ouabain-digoxin antagonism in rat arteries and neurones. J Physiol. 2014 Mar 1;592(5):941-69. doi: 10.1113/jphysiol.2013.266866. Erratum in: J Physiol. 2014 Nov 1;592(Pt 21):4803. PubMed PMID: 24344167; PubMed Central PMCID: PMC3948557. 5: Wenceslau CF, Rossoni LV. Rostafuroxin ameliorates endothelial dysfunction and oxidative stress in resistance arteries from deoxycorticosterone acetate-salt hypertensive rats: the role of Na+K+-ATPase/ cSRC pathway. J Hypertens. 2014 Mar;32(3):542-54. doi: 10.1097/HJH.0000000000000059. PubMed PMID: 24309491. 6: Kirshenbaum GS, Clapcote SJ, Duffy S, Burgess CR, Petersen J, Jarowek KJ, Yücel YH, Cortez MA, Snead OC 3rd, Vilsen B, Peever JH, Ralph MR, Roder JC. Mania-like behavior induced by genetic dysfunction of the neuron-specific Na+,K+-ATPase α3 sodium pump. Proc Natl Acad Sci U S A. 2011 Nov 1;108(44):18144-9. doi: 10.1073/pnas.1108416108. Erratum in: Proc Natl Acad Sci U S A. 2012 Feb 7;109(6):2174. PubMed PMID: 22025725; PubMed Central PMCID: PMC3207708. 7: Staessen JA, Thijs L, Stolarz-Skrzypek K, Bacchieri A, Barton J, Espositi ED, de Leeuw PW, Dłużniewski M, Glorioso N, Januszewicz A, Manunta P, Milyagin V, Nikitin Y, Souček M, Lanzani C, Citterio L, Timio M, Tykarski A, Ferrari P, Valentini G, Kawecka-Jaszcz K, Bianchi G. Main results of the ouabain and adducin for Specific Intervention on Sodium in Hypertension Trial (OASIS-HT): a randomized placebo-controlled phase-2 dose-finding study of rostafuroxin. Trials. 2011 Jan 14;12:13. doi: 10.1186/1745-6215-12-13. PubMed PMID: 21235787; PubMed Central PMCID: PMC3031200. 8: Lanzani C, Citterio L, Glorioso N, Manunta P, Tripodi G, Salvi E, Carpini SD, Ferrandi M, Messaggio E, Staessen JA, Cusi D, Macciardi F, Argiolas G, Valentini G, Ferrari P, Bianchi G. Adducin- and ouabain-related gene variants predict the antihypertensive activity of rostafuroxin, part 2: clinical studies. Sci Transl Med. 2010 Nov 24;2(59):59ra87. doi: 10.1126/scitranslmed.3001814. PubMed PMID: 21106941. 9: Ferrandi M, Molinari I, Torielli L, Padoani G, Salardi S, Rastaldi MP, Ferrari P, Bianchi G. Adducin- and ouabain-related gene variants predict the antihypertensive activity of rostafuroxin, part 1: experimental studies. Sci Transl Med. 2010 Nov 24;2(59):59ra86. doi: 10.1126/scitranslmed.3001815. PubMed PMID: 21106940. 10: Citterio L, Lanzani C, Manunta P, Bianchi G. Genetics of primary hypertension: the clinical impact of adducin polymorphisms. Biochim Biophys Acta. 2010 Dec;1802(12):1285-98. doi: 10.1016/j.bbadis.2010.03.014. Review. PubMed PMID: 20382219. 11: Ferrari P. Rostafuroxin: an ouabain-inhibitor counteracting specific forms of hypertension. Biochim Biophys Acta. 2010 Dec;1802(12):1254-8. doi: 10.1016/j.bbadis.2010.01.009. Review. PubMed PMID: 20083196. 12: Schoner W, Scheiner-Bobis G. Endogenous and exogenous cardiac glycosides and their mechanisms of action. Am J Cardiovasc Drugs. 2007;7(3):173-89. Review. PubMed PMID: 17610345. 13: Ferrandi M, Molinari I, Bianchi G, Ferrari P. Ouabain-dependent signaling in caveolae as a novel therapeutic target for hypertension. Cell Mol Biol (Noisy-le-grand). 2006 Dec 30;52(8):15-8. Review. PubMed PMID: 17535730. 14: Schoner W, Scheiner-Bobis G. Endogenous and exogenous cardiac glycosides: their roles in hypertension, salt metabolism, and cell growth. Am J Physiol Cell Physiol. 2007 Aug;293(2):C509-36. Review. PubMed PMID: 17494630. 15: Ferrari P, Ferrandi M, Valentini G, Manunta P, Bianchi G. Targeting Ouabain- and Adducin-dependent mechanisms of hypertension and cardiovascular remodeling as a novel pharmacological approach. Med Hypotheses. 2007;68(6):1307-14. PubMed PMID: 17097240. 16: Iwamoto T, Kita S. Hypertension, Na+/Ca2+ exchanger, and Na+, K+-ATPase. Kidney Int. 2006 Jun;69(12):2148-54. Review. PubMed PMID: 16641927. 17: Manunta P, Ferrandi M, Messaggio E, Ferrari P. A new antihypertensive agent that antagonizes the prohypertensive effect of endogenous ouabain and adducin. Cardiovasc Hematol Agents Med Chem. 2006 Jan;4(1):61-6. Review. PubMed PMID: 16529550. 18: Ferrari P, Ferrandi M, Valentini G, Bianchi G. Rostafuroxin: an ouabain antagonist that corrects renal and vascular Na+-K+- ATPase alterations in ouabain and adducin-dependent hypertension. Am J Physiol Regul Integr Comp Physiol. 2006 Mar;290(3):R529-35. Review. PubMed PMID: 16467500. 19: Ferrandi M, Barassi P, Molinari I, Torielli L, Tripodi G, Minotti E, Bianchi G, Ferrari P. Ouabain antagonists as antihypertensive agents. Curr Pharm Des. 2005;11(25):3301-5. Review. PubMed PMID: 16250857. 20: Staessen JA, Kuznetsova T, Acceto R, Bacchieri A, Brand E, Burnier M, Celis H, Citterio L, de Leeuw PW, Filipovský J, Fournier A, Kawecka-Jaszcz K, Manunta P, Nikitin Y, O'Brien ET, Redón J, Thijs L, Ferrari P, Valentini G, Bianchi G. OASIS-HT: design of a pharmacogenomic dose-finding study. Pharmacogenomics. 2005 Oct;6(7):755-75. PubMed PMID: 16207152.