Rostafuroxin  ≥98%

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包装规格:5mg 25mg 100mg in glass bottle
溶解性:溶于DMSO(≥50mg/mL )
产品描述:基本信息 产品编号: R10157 产品名称: Rostafuroxin CAS: 156722-18-8   储存条件 粉末 -20℃ 四年     分子式: C23H34O4 溶于液体 -80℃ 6个月 分子量: 374.52 -20℃ 1个月 化学名:  3S,5R,8R,9S,10S,13S,14S,17S)-17-(furan-3-yl)-10,13-dimethylhexadecahydro-14H-cyclopenta[a]phenanthrene-3,14,17-triol Solubility (25°C):   体外:   DMSO   Ethanol   Water   体内(现配现用):   <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.6702mL 13.3508mL 26.7016mL 5mM 0.5340mL 2.6702mL 5.3403mL 10mM 0.2670mL 1.3351mL 2.6702mL   生物活性 产品描述 一种Na+K ATPase拮抗剂。 靶点 Na+/K+ATPase;RSV   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 (0.125-128μM;for 24h 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=1.8μM) and A549 cells (IC50=14.8μM).Rostafuroxin displaced [3H]Ouabain from the dog kidney Na+,K+-ATPase receptor (IC50=1.5nM),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;1mg/kg/day;gavage;for 3 weeks) decreases SBP and improves acetylcholine-induced relaxation. Animal Model: Male 7-week-old Wistar rats Dosage: 1mg/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.
保存条件:-20℃