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Rostafuroxin

Cat. No. M3696

Rostafuroxin Structure

Synonym: PST 2238

Size Price Availability Quantity
5mg USD 90 In stock
10mg USD 135 In stock
50mg USD 585 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 374.51
Formula C23H34O4
CAS Number 156722-18-8
Purity >99%
Solubility DMSO
Storage at -20°C
References

Rostafuroxin protects from podocyte injury and proteinuria induced by adducin genetic variants and ouabain.
Ferrandi M, et al. J Pharmacol Exp Ther. 2014 Nov;351(2):278-87. PMID: 25187430.

Rostafuroxin: an ouabain-inhibitor counteracting specific forms of hypertension.
Ferrari P. Biochim Biophys Acta. 2010 Dec;1802(12):1254-8. PMID: 20083196.

Rostafuroxin: an ouabain antagonist that corrects renal and vascular Na+-K+- ATPase alterations in ouabain and adducin-dependent hypertension.
Ferrari P, et al. Am J Physiol Regul Integr Comp Physiol. 2006 Mar;290(3):R529-35. PMID: 16467500.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Rostafuroxin, PST 2238 supplier, ATPase, inhibitors

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