| 货号 | 21282-1mg |
| 描述 | Rostafuroxin potently inhibits binding of endogenous ouabain to the Na+/K+ ATPase (IC50 = 1.7 µM) through the Src-epidermal growth factor receptor (EGFR)-dependent signaling pathway.1 This blocks the ouabain-dependent increase in Na+/K+ ATPase activity. In cultured renal cells where the Na+/K+ ATPase is upregulated or has increased activity, rostafuroxin normalizes mRNA levels and Na+/K+ ATPase activity.2 At very low doses (1 and 10 µg/kg for 5-6 weeks) in Milan-hypertensive rats, it decreased the development of hypertension.3 In a Phase II clinical study, rostafuroxin did not reduce blood pressure in human patients at doses of 0.05-5.0 mg/d.4 |
| 别名 | PST 2238; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Ferrari, P.,Ferrandi, M.,Valentini, G., et al. 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. 290(3), R529-R535 (2006). 2.Ferrari, P.,Torielli, L.,Ferrandi, M., et al. PST2238: A new antihypertensive compound that antagonizes the long-term pressor effect of ouabain. J. Pharmacol. Exp. Ther. 285(1), 83-94 (1998). 3.Ferrari, P.,Ferrandi, M.,Tripodi, G., et al. PST 2238: A new antihypertensive compound that modulates Na,K-ATPase in genetic hypertension. J. Pharmacol. Exp. Ther. 288(3), 1074-1083 (1999). 4.Staessen, J.A.,Thijs, L.,Stolarz-Skrzypek, K., et al. Main results of the ouabain and adducin for specific intervention on sodium in hypertension trial (OASIS-HT): A randomized placebo-controlled phase-2 dose-finding study of rostafuroxin. Trials 12, 13 (2011). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 374.5 |
| 分子式 | C23H34O4 |
| CAS号 | 156722-18-8 |
| 稳定性 | ≥ 2 years |
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