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Istaroxime hydrochloride  ≥98%

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包装规格：2mg 5mg 10mg 50mg 100mg in glass bottle
溶解性：溶于DMSO(≥45mg/ml)
产品描述：基本信息 产品编号： I10346 产品名称： Istaroxime hydrochloride CAS: 374559-48-5   储存条件 粉末 -20℃ 四年     分子式： C21H33ClN2O3 溶于液体 -80℃ 6个月 分子量： 396.95 -20℃ 1个月 化学名：  UNII-N24U08609A component AXHJYJDJXNOGNI-ROJIRLEOSA-N 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 2.5192mL 12.5960mL 25.1921mL 5mM 0.5038mL 2.5192mL 5.0384mL 10mM 0.2519mL 1.2596mL 2.5192mL   生物活性 产品描述 Na+/K+-ATPase抑制剂(IC50=0.11μM)和肌浆/内质网钙ATP酶2(SERCA2)激活剂。 靶点 IC50:0.11μM (Na+,K+-ATPase)   体外研究 Istaroxime hydrochloride acting as a positive inotropic compound through the inhibition of the Na+,K+-ATPase.Istaroxime (PST2744) inhibits the Na+/K+-ATPase activity from dog kidney with an IC50 value of 0.43±0.15μM.Inhibition of Na+/K+-ATPase activity in preparations from guinea pig kidney yielded potencies of 8.5μM 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±0.37mg/kg and a peak of 140±3.5% at the dose (EDmax) of 4.88±0.6mg/kg.   推荐实验方法(仅供参考) 激酶实验： Dog or guinea pig kidney outer medulla is homogenized with a Polytron in 250mM sucrose and 30mM histidine,at pH 7.2.The homogenate is centrifuged at 6,000g for 15 min at 4℃ and the supernatant at 48,000g for 30 min at 20℃ with SDS and then layered onto a discontinuous sucrose density gradient (10,15,and 29%) and centrifuged at 60,000 rpm for 115 min at 4℃.The pellet is resuspended in 25mM imidazole and 1mM EDTA,pH 7.5. Protein content is measured.Na+/K+-ATPase activity is measured after the release of 32P from [32P]ATP.Increasing concentrations of compounds are preincubated with purified enzyme for 10 min at 37℃ in 120μL of final volume of medium containing 140mM NaCl,3mM MgCl2,50mM HEPESTris,and 3mM ATP,pH 7.5.After preincubation,10μL of incubation solution containing 10mM KCl and 20 nCi of [32P]ATP (0.5-3 Ci/mmol) is added,and the reaction is carried out for 15 min at 37℃ before being stopped by acidification with 30% (v/v) perchloric acid.32P is separated by centrifugation with activated charcoal and radioactivity measured by liquid scintillation counting.Inhibitory activity is expressed as percentage of control sample,carried out in the absence of standard compound.IC50 is calculated by weighed nonlinear regression curve fitting to the mass-action equilibrium.   动物实验:   Pigs Male guinea Pigs (350-450g) are used.Istaroxime (300μg/kg) or Digoxin (75μg/kg) are given by i.v.bolus 10 and 20 min before starting the exercise,respectively,and compared with vehicle.The following variables,HR,ECG,LVP,and aortic pressures,are recorded through a computerized acquisition system,which calculated the left ventricular rates of pressure changes.Data are analyzed from the real-time digitized recordings.Control values are obtained before compound administration.
保存条件：-20℃

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