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Rostafuroxin

目录号 M3696 所有产品仅供科研使用,严禁用于人或动物的治疗等任何其他用途,不为任何个人提供产品和服务  


rostafuroxin, a novel antihypertensive agent developed as a selective inhibitor of Src-SH2 interaction with mutant adducin- and ouabain-activated Na,K-ATPase

Rostafuroxin结构式

别名:PST 2238

包装 价格 库存状态
5mg 原价 ¥ 900
促销价 ¥ 855
中国库存现货
10mg 原价 ¥ 1350
促销价 ¥ 1282.5
中国库存现货
50mg 原价 ¥ 5850
促销价 ¥ 5557.5
中国库存现货
其他规格数量报价?

质量控制及产品安全说明书
  • 当前批次:
  • 纯度 >98%
  • COA
  • MSDS
生物活性

Rostafuroxin (PST 2238) is a new oral antihypertensive agent able to selectively antagonize EO, adducin pressor, and molecular effects. It is endowed with high potency and efficacy in reducing blood pressure and preventing organ hypertrophy in animal models representative of both adducin and EO mechanisms.At molecular level, in the kidney, Rostafuroxin antagonizes EO triggering of the Src-epidermal growth factor receptor (EGFr)-dependent signaling pathway leading to renal Na+-K+ pump, and ERK tyrosine phosphorylation and activation.In the vasculature, it normalizes the increased myogenic tone caused by nanomolar ouabain. A very high safety ratio and an absence of interaction with other mechanisms involved in blood pressure regulation, together with initial evidence of high tolerability and efficacy in hypertensive patients, indicate Rostafuroxin as the first example of a new class of antihypertensive agents designed to antagonize adducin and EO-hypertensive mechanisms.

不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)
小鼠 大鼠 豚鼠 仓鼠
重量 (kg) 0.02 0.15 1.8 0.4 0.08 10
体表面积 (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km 系数 3 6 12 8 5 20
动物 A (mg/kg) = 动物 B (mg/kg) ×  动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将白藜芦醇用于小鼠的剂量22.4 mg/kg 换算成大鼠的剂量,需要将22.4 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到白藜芦醇用于大鼠的等效剂量为11.2 mg/kg。

化学数据
分子量 374.51
分子式 C23H34O4
CAS号 156722-18-8
纯度 >98%
溶解性(25°C) DMSO
储存和运输条件 固体粉末: -20°C 冷藏长期储存
常温运输及临时存放
储备液配制

以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.6702 mL 13.3508 mL 26.7016 mL
5 mM 0.534 mL 2.6702 mL 5.3403 mL
10 mM 0.267 mL 1.3351 mL 2.6702 mL
参考文献

Rostafuroxin protects from podocyte injury and proteinuria induced by adducin genetic variants and ouabain.
Ferrandi M, et al. J Pharmacol Exp Ther. 2014 Nov;351(2):278-87. PMID: 25187430.

Rostafuroxin: an ouabain-inhibitor counteracting specific forms of hypertension.
Ferrari P. Biochim Biophys Acta. 2010 Dec;1802(12):1254-8. PMID: 20083196.

Rostafuroxin: an ouabain antagonist that corrects renal and vascular Na+-K+- ATPase alterations in ouabain and adducin-dependent hypertension.
Ferrari P, et al. Am J Physiol Regul Integr Comp Physiol. 2006 Mar;290(3):R529-35. PMID: 16467500.

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