Rostafuroxin (PST 2238)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50:对Na+-K+-ATPase 的IC50为2 μM.
在高血压中观察到两种机制参与决定管状Na+重吸收的异常:细胞骨架蛋白α内收蛋白的多态性以及循环内源性哇巴因(EO)水平的增加.这两种机制均导致肾Na+-K+泵的活性和表达增加,肾Na+-K+泵是管状Na运输的驱动力.血管形态和功能的改变也与EO相关.Rostafuroxin (PST 2238)能够选择性地拮抗EO\内收升压和分子效应,是新型的口服抗高血压剂.
体外实验:在分子水平上,在肾脏中,rostafuroxin通过引发Src-表皮生长因子受体(EGFr)依赖的信号传导途径,从而导致肾Na+-K+泵\ERK酪氨酸磷酸化和激活,进而拮抗EO.在脉管系统中,rostafuroxin可以使纳摩尔哇巴因引起的肌原性紧张增加恢复正常化[1].
在体实验:在MHS大鼠中,口服给药剂量为1到100 μg/kg/day的rostafuroxin可以降低血压,但不影响心率,恢复肾脏Na+-K+-ATPase的正常活性.同样,rostafuroxin促进NUA大鼠的血压恢复正常[1].
临床试验:Rostafuroxin在I期研究中已经满足安全要求,单次或重复给药剂量达10 mg/day的Rostafuroxin具有完全耐受性,与安慰剂相比没有表现出副作用差异.在轻度高血压并发症患者的两个探索性研究中,口服剂量为0.1到1 mg/day的rostafuroxin可以有效地降低血压[1].
参考文献:
[1] Ferrari P, Ferrandi M, Valentini G, Bianchi G. Rostafuroxin: an ouabain antagonist that corrects renal and vascular Na+-K+-ATPase alterations in ouabain and adducin-dependent hypertension. Am J Physiol Regul Integr Comp Physiol. 2006 Mar;290(3):R529-35.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 374.51 |
Cas No. | 156722-18-8 |
Formula | C23H34O4 |
Solubility | insoluble in H2O; insoluble in EtOH; ≥12.05 mg/mL in DMSO |
Chemical Name | (3S,5R,8R,9S,10S,13S,14S,17S)-17-(furan-3-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthrene-3,14,17-triol |
SDF | Download SDF |
Canonical SMILES | C[C@]12CC[C@@](O)([H])C[C@@]1([H])CC[C@]3([H])[C@]2([H])CC[C@@]4([C@](C5=COC=C5)(O)CC[C@]34O)C |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |