156722-18-8
156722-18-8 結(jié)構(gòu)式
基本信息
PST2238
17-triol
AC1L4BGU
Rostafuroxin
CHEMBL2068971
SureCN1716210
UNII-P848LCX62B
PST 2238, >=98%
PST2238,Rostafuroxin
物理化學(xué)性質(zhì)
常見問(wèn)題列表
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.
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. |