Rostafuroxin

SKU: orb1226093

Description

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.Hypertension Phase 2 Clinical(In Vitro):Rostafuroxin (PST 2238) competitively inhibits Ouabain (HY-B0542) binding and signaling. Rostafuroxin antagonizes the molecularand functional effects of Ouabain by reversing the ouabain-induced, Src-dependent Na+,K+-ATPase phosphorylation and activation.Rostafuroxin (0.125-128 μM; for 24 h post treatment) has less than 20% reduction in cell viability in A549 cells and HSAEC. Rostafuroxin inhibits the expression of RSV-GFP in HSAEC (IC50=1.8 μM) and A549 cells (IC50=14.8 μM).Rostafuroxin displaced [3H]Ouabain from the dog kidney Na+,K+-ATPase receptor (IC50=1.5 nM), is devoid of cardiac inotropic activity in isolated guinea pig atria, and shows no affinity up to 10-4 M with general (R1, R2, a1, a2, A1, A2, M1, M2, H1, H2, 5-HT1, 5-HT2, Ca2+ channels, TXA2/PGH2, PAF, GABAA, GABAB, DA-NE-5-HT uptake, glutammate,glycine, benzodiazepine) and hormonal (estrogenic, progestinic, androgenic, mineralcorticoid) receptors.(In Vivo):Rostafuroxin (PST 2238; 1 mg/kg/day; gavage; for 3 weeks) decreases SBP and improves acetylcholine-induced relaxation.

Key Properties

• CAS Number: 156722-18-8
• MW: 374.5137
• Purity: >98% (HPLC)
• Formula: C₂₃H₃₄O₄
• SMILES: 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
• Target: Na-K-ATPase
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  Rostafuroxin (PST 2238; 1 mg/kg/day; gavage; for 3 weeks) decreases SBP and improves acetylcholine-induced relaxation. Animal model: Male 7-week-old Wistar rats. Dosage: 1 mg/kg. Administration: Gavage; daily; for 3 weeks. Result: Decreased SBP, improved acetylcholine-induced relaxation via enhanced nitric oxide synthesis and bioavailability, decreased superoxide anion generation from NAD(P)H oxidase and cyclooxygenase-2 and reduced cytoplasmic tyrosine kinase Src phosphorylation.
• In Vitro:
  Rostafuroxin (PST 2238) competitively inhibits Ouabain (HY-B0542) binding and signaling. Rostafuroxin antagonizes the molecularand functional effects of Ouabain by reversing the ouabain-induced, Src-dependent Na+, K+-ATPase phosphorylation and activation. Rostafuroxin (0.125-128 μM; for 24 h post treatment) has less than 20% reduction in cell viability in A549 cells and HSAEC. Rostafuroxin inhibits the expression of RSV-GFP in HSAEC (IC50 = 1.8 μM) and A549 cells (IC50 = 14.8 μM). Rostafuroxin displaced [3H]Ouabain from the dog kidney Na+, K+-ATPase receptor (IC50 = 1.5 nM), is devoid of cardiac inotropic activity in isolated guinea pig atria, and shows no affinity up to 10-4 M with general (R1, R2, a1, a2, A1, A2, M1, M2, H1, H2, 5-HT1, 5-HT2, Ca2+ channels, TXA2/PGH2, PAF, GABAA, GABAB, DA-NE-5-HT uptake, glutammate, glycine, benzodiazepine) and hormonal (estrogenic, progestinic, androgenic, mineralcorticoid) receptors.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PST-2238 | PST2238 | PST 2238

Quick Database Links

Gene Symbol

Na-K-ATPase