ROSTAFUROXIN
| 中文名称 | ROSTAFUROXIN |
|---|---|
| 中文同义词 | (3Β,?5Β,?14Β)?-?21,23-环氧-24-降胆固醇-20,22-二烯-3,14,17-三醇;化合物ROSTAFUROXIN;(3S,5R,8R,9S,10S,13S,14S,17S)-17-(呋喃-3-基)-10,13-二甲基十六氢-1H-环戊二烯并[A]菲-3,14,17-三醇 |
| 英文名称 | (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 |
| 英文同义词 | (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;Rostafuroxin;PST2238;(3β,5β,14β)-21,23-Epoxy-24-Norchola-20,22-diene-3,14,17-triol;Rostafuroxin (PST-2238);(3beta,5beta,14beta)-21,23-Epoxy-24-norchola-20,22-diene-3,14,17-triol;Rostafuroxin PST2284;(3beta,5beta,14beta)-21,23-Epoxy-24-norchola-20,22-diene-3,14,17-triol Rostafuroxin (PST 2238) |
| CAS号 | 156722-18-8 |
| 分子式 | C23H34O4 |
| 分子量 | 374.51 |
| EINECS号 | |
| 相关类别 | 小分子抑制剂，天然产物;小分子抑制剂;Inhibitors |
| Mol文件 | 156722-18-8.mol |
| 结构式 |  |
ROSTAFUROXIN 性质
| 沸点 | 451.3±45.0 °C(Predicted) |
|---|---|
| 密度 | 1.226±0.06 g/cm3(Predicted) |
| 储存条件 | Sealed in dry,Store in freezer, under -20°C |
| 溶解度 | 不溶于水；不溶于乙醇； ≥12.05 mg/mL，溶于 DMSO |
| 形态 | 固体 |
| 酸度系数(pKa) | 14.02±0.70(Predicted) |
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. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-12283 | Rostafuroxin | 1 mg | 300元 | |
| 2024/01/25 | HY-12283 | ROSTAFUROXIN Rostafuroxin | 156722-18-8 | 5mg | 750元 |