S85142 |
Istaroxime (hydrochloride) |
源叶(MedMol) | 99% |
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- 产品描述: Istaroxime hydrochloride is a Na+/K+-ATPase inhibitor (IC50=0.11 μM) and a sarcoplasmic/endoplasmic reticulum calcium ATPase 2 (SERCA 2) activator.
- 靶点: IC50: 0.11 μM (Na+,K+-ATPase)
- 体外研究:
Istaroxime hydrochloride acting as a positive inotropic compound through the inhibition of the Na+,K+-ATPase[2]. Istaroxime (PST2744) inhibits the Na+/K+-ATPase activity from dog kidney with an IC50 value of 0.43 ± 0.15 μM. Inhibition of Na+/K+-ATPase activity in preparations from guinea pig kidney yielded potencies of 8.5 μM for PST2744
- 体内研究:
Istaroxime (PST2744) induces a progressive increase in +dP/dtmax throughout the infusion that reaches 80% (ED80) at the cumulative dose of 1.89±0.37 mg/kg and a peak of 140±3.5% at the dose (EDmax) of 4.88±0.6 mg/kg
- 参考文献:
1. Gobbini M, et al. Novel analogues of istaroxime, a potent inhibitor of Na+,K+-ATPase: synthesis and structure-activity relationship. J Med Chem. 2008 Aug 14;51(15):4601-8. 2. Gobbini M, et al. Novel analogues of Istaroxime, a potent inhibitor of Na(+),K(+)-ATPase: Synthesis, structure-activity relationship and 3D-quantitative structure-activity relationship of derivatives at position 6 on the androstane scaffold. Bioorg Med Chem. 2010 Jun 15;18(12):4275-99. 3. Micheletti R, et al. Pharmacological profile of the novel inotropic agent (E,Z)-3-((2-aminoethoxy)imino)androstane-6,17-dione hydrochloride (PST2744). J Pharmacol Exp Ther. 2002 Nov;303(2):592-600.
- 溶解性: Soluble in DMSO、H2O
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.519 ml 12.596 ml 25.192 ml 5 mM 0.504 ml 2.519 ml 5.038 ml 10 mM 0.252 ml 1.26 ml 2.519 ml 50 mM 0.05 ml 0.252 ml 0.504 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)