| Bioactivity | Rostafuroxin (PST 2238), a digitoxigenin derivative, is an orally active and potent Na+,K+-ATPase (ATP1A1) antognist. Rostafuroxin binds specifically to the ATP1A1 extracellular domain and blocks respiratory syncytial virus (RSV)-triggered EGFR Tyr845 phosphorylation. Rostafuroxin has antihypertensive and anti-RSV activity[1][2][3][4]. | ||||||||||||
| Invitro | 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[3][4]. 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)[3]. 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[1]. | ||||||||||||
| In Vivo | Rostafuroxin (PST 2238; 1 mg/kg/day; gavage; for 3 weeks) decreases SBP and improves acetylcholine-induced relaxation[4]. Animal Model: | ||||||||||||
| Name | Rostafuroxin | ||||||||||||
| CAS | 156722-18-8 | ||||||||||||
| Formula | C23H34O4 | ||||||||||||
| Molar Mass | 374.51 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|
||||||||||||
| Reference | [1]. Quadri L, et al. 17 beta-(3-furyl)-5 beta-androstane-3 beta, 14 beta, 17 alpha-triol (PST 2238). A very potent antihypertensive agent with a novel mechanism of action. J Med Chem. 1997 May 23;40(11):1561-4. [2]. Ferrari P, et al. PST 2238: A new antihypertensive compound that modulates Na,K-ATPase in genetic hypertension. J Pharmacol Exp Ther. 1999 Mar;288(3):1074-83. [3]. Matthias Lingemann, et al. The alpha-1 subunit of the Na+,K+-ATPase (ATP1A1) is required for macropinocytic entry of respiratory syncytial virus (RSV) in human respiratory epithelial cells. PLoS Pathog. 2019 Aug 5;15(8):e1007963. [4]. Camilla F Wenceslau, et al. 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. 20 |
Rostafuroxin
CAS: 156722-18-8 F: C23H34O4 W: 374.51
Rostafuroxin (PST 2238), a digitoxigenin derivative, is an orally active and potent Na+,K+-ATPase (ATP1A1) antognist. Ro
Sales Email：peptidedb@qq.com
This product is for research use only, not for human use. We do not sell to patients.