An endogenous ouabain blocker at the Na+/K+ ATPase
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Rostafuroxin

Item No. 21282

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(3β,5β,14β)-21,23-epoxy-24-norchola-20,22-diene-3,14,17-triol
CAS Number
156722-18-8
Synonyms
  • PST 2238
Molecular Formula
C23H34O4
Formula Weight
374.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 2 mg/mlDMSO: 0.1 mg/mlEthanol: 20 mg/mlEthanol:PBS (pH 7.2)(1:2): 0.3 mg/ml
λmax
212 nm
SMILES
O[C@H]1CC[C@@]2(C)[C@@](CC[C@]3([H])[C@]2([H])CC[C@@]4(C)[C@]3(O)CC[C@]4(O)C5=COC=C5)([H])C1
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
InChi Key
AEAPORIZZWBIEX-DTBDINHYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    Rostafuroxin potently inhibits binding of endogenous ouabain to the Na+/K+ ATPase (IC50 = 1.7 µM) through the Src-epidermal growth factor receptor (EGFR)-dependent signaling pathway.1 This blocks the ouabain-dependent increase in Na+/K+ ATPase activity. In cultured renal cells where the Na+/K+ ATPase is upregulated or has increased activity, rostafuroxin normalizes mRNA levels and Na+/K+ ATPase activity.2 At very low doses (1 and 10 µg/kg for 5-6 weeks) in Milan-hypertensive rats, it decreased the development of hypertension.3 In a Phase II clinical study, rostafuroxin did not reduce blood pressure in human patients at doses of 0.05-5.0 mg/d.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ferrari, P., Ferrandi, M., Valentini, G., et al. 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. 290(3), R529-R535 (2006).

    2. Ferrari, P., Torielli, L., Ferrandi, M., et al. PST2238: A new antihypertensive compound that antagonizes the long-term pressor effect of ouabain. J. Pharmacol. Exp. Ther. 285(1), 83-94 (1998).

    3. Ferrari, P., Ferrandi, M., Tripodi, G., et al. PST 2238: A new antihypertensive compound that modulates Na,K-ATPase in genetic hypertension. J. Pharmacol. Exp. Ther. 28893, 1074-1083 (1999).

    4. Staessen, J.A., Thijs, L., Stolarz-Skrzypek, K., et al. 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 12, 13 (2011).