Rostafuroxin

Rostafuroxin - Names and Identifiers

Name	(3β,5β,14β)-21,23-Epoxy-24-Norchola-20,22-diene-3,14,17-triol
Synonyms	PST2238 ROSTAFUROXIN Rostafuroxin Rostafuroxin PST2284 Rostafuroxin (PST-2238) (3β,5β,14β)-21,23-Epoxy-24-Norchola-20,22-diene-3,14,17-triol (3beta,5beta,14beta)-21,23-Epoxy-24-norchola-20,22-diene-3,14,17-triol (3beta,5beta,14beta)-21,23-Epoxy-24-norchola-20,22-diene-3,14,17-triol Rostafuroxin (PST 2238) (3S,5R,8R,9S,10S,13R,14S,17R)-17-(3-furyl)-10,13-dimethyl-2,3,4,5,6,7, 8,9,11,12,15,16-dodecahydro-1H-cyclopenta[a]phenanthrene-3,14,17-triol
CAS	156722-18-8

Rostafuroxin - Physico-chemical Properties

Molecular Formula	C23H34O4
Molar Mass	374.51
Density	1.226±0.06 g/cm3(Predicted)
Boling Point	451.3±45.0 °C(Predicted)
pKa	14.02±0.70(Predicted)
Storage Condition	Sealed in dry,Store in freezer, under -20°C
In vitro study	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 (IC 50 =1.8 μM) and A549 cells (IC 50 =14.8 μM). Rostafuroxin displaced [ 3 H]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 study	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.