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156722-18-8

中文名称 ROSTAFUROXIN
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
CAS 156722-18-8
分子式 C23H34O4
分子量 374.51
MOL 文件 156722-18-8.mol
更新日期 2024/04/28 11:56:10
156722-18-8 结构式 156722-18-8 结构式

基本信息

中文别名
(3Β,?5Β,?14Β)?-?21,23-环氧-24-降胆固醇-20,22-二烯-3,14,17-三醇
英文别名
CS-906
PST2238
17-triol
AC1L4BGU
Rostafuroxin
CHEMBL2068971
SureCN1716210
UNII-P848LCX62B
PST 2238, >=98%
PST2238,Rostafuroxin
所属类别
生物化工:激动剂抑制剂

物理化学性质

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insoluble in H2O; insoluble in EtOH; ≥12.05 mg/mL in DMSO
酸度系数(pKa)14.02±0.70(Predicted)
形态固体
ROSTAFUROXIN价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2024/04/30HY-12283ROSTAFUROXIN
Rostafuroxin
156722-18-85mg750元
2024/04/30HY-12283ROSTAFUROXIN
Rostafuroxin
156722-18-810mM * 1mLin DMSO830元
2024/04/30HY-12283ROSTAFUROXIN
Rostafuroxin
156722-18-810mg1350元

常见问题列表

生物活性
Rostafuroxin (PST 2238) 是一种洋地黄毒苷衍生物,一种口服有效的 Na+,K+-ATPase (ATP1A1) 抑制剂。Rostafuroxin 与 ATP1A1 胞外域特异性结合,并阻断呼吸道合胞病毒 (RSV) 触发的 EGFR Tyr845 磷酸化。Rostafuroxin 具有抗高血压和抗 RSV 活性。
体外研究

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.

体内研究

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.
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