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Istaroxime hydrochloride

现货
Catalog No.
A3508
Na+ / K+ ATPase的抑制剂
组合的产品项目
规格价格库存 数量
2mg
¥ 1,580.00
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5mg
¥ 2,370.00
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10mg
¥ 3,630.00
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50mg
¥ 10,180.00
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100mg
¥ 15,400.00
Ship with 10-15 days

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Background

Istaroxime hydrochloride(PST2744) is a novel inhibitor of Na+/K+-ATPase with IC50 value of 0.43±0.15μM [1].

In vitro studies show that Istaroxime can inhibit the activity of Na+/K+-ATPase from dog kidney without significant interaction with other several receptors. It demonstrates the selectivity of Istaroxime. Ex vivo studies show the inotropic effect can be achieved up to 60% for Istaroxime. Istaroxime can also increase the force of contraction of guinea pig paced left atria in the range 0.3 to 30μM. In vivo assays prove Istaroxime is consistently safer than digoxin [1].

Istaroxime is a steroidal drug unrelated to cardiac glycosides that improves cellular calcium cycling. The inhibition of Na+/K+-ATPase induces cytosolic calcium accumulation during systole (inotropism). Clinical studies has been done with istaroxime in phase II. Istaroxime could be a promising alternative for patients with acute heart failure syndrome for whom the therapeutic options are currently limited [2].

References:
[1] R. Micheletti, G. G. Mattera, M. Rocchetti, A. Schiavone, M. F. Loi, A. Zaza, R. J. P. Gagnol, S. De Munari, P. Melloni, P. Carminati, G. Bianchi, and P. Ferrari. Pharmacological profile of the novel inotropic agent (e,z)-3-((2-aminoethoxy)imino)androstane-6,17-dione hydrochloride (PST2744). The journal of pharmacology and experimental therapeutics. 2002, 303 (2): 592-600.
[2] Suruchi Aditya, Aditya Rattan. Istaroxime: A rising star in acute heart failure. Journal of Pharmacology and Pharmacotherapeutics. 2012, 3(4): 353-355.

Chemical Properties

StorageStore at -20°C
M.Wt396.95
Cas No.374559-48-5
FormulaC21H33ClN2O3
SynonymsPST-2744 (hydrochloride);PST 2744 (hydrochloride);PST2744 (hydrochloride)
SolubilitySoluble in DMSO
Chemical Name(5S,8R,9S,10R,13S,14S)-3-(2-aminoethoxyimino)-10,13-dimethyl-1,2,4,5,7,8,9,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthrene-6,17-dione;hydrochloride
SDFDownload SDF
Canonical SMILESCC12CCC(=NOCCN)CC1C(=O)CC3C2CCC4(C3CCC4=O)C.Cl
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。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。

试验操作

细胞实验[1]:

细胞系

豚鼠心室肌细胞

溶解方法

该化合物在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月

反应条件

4 μM,0.5 s

实验结果

Istaroxime(从61.3到92.4 nM)增加静息Ca2+的程度相似。Istaroxime使[Ca]SR-tot增加47%。在咖啡因诱导瞬变期间(+130),Istaroxime增加通过Na+/Ca2+交换器(CaNCX)的Ca2+量。Istaroxime缩短了咖啡因脉冲开始和SRCa2+释放之间的时间。

动物实验[2]:

动物模型

Bio TO.2仓鼠和Bio F1B仓鼠

剂量

口服,30 mg/5mL/kg/day

实验结果

Istaroxime治疗的仓鼠的心脏功能与健康动物相当,与对照处理的动物相比,Istaroxime显著提高LVSP以及阳性和阴性dP/dT。与对照组处理的Bio TO.2动物相比,从istroxime处理的仓鼠分离的心脏冠状动脉流速较大。此外,与对照组动物相比,istaroxime处理的Bio TO.2仓鼠具有HRV的时间和频率域指数,即R-R间期、TP、LF和HF的标准偏差。此外,istaroxime处理的动物的LF/HF比率与在Bio F1B仓鼠中观察到的相似。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1] Rocchetti M, Besana A, Mostacciuolo G, et al. Modulation of sarcoplasmic reticulum function by Na+/K+ pump inhibitors with different toxicity: digoxin and PST2744 [(E, Z)-3-((2-aminoethoxy) imino) androstane-6, 17-dione hydrochloride]. Journal of Pharmacology and Experimental Therapeutics, 2005, 313(1): 207-215.

[2] Giudice P L, Mattera G G, Gagnol J P, et al. Chronic istaroxime improves cardiac function and heart rate variability in cardiomyopathic hamsters. Cardiovascular drugs and therapy, 2011, 25(2): 133-138.

生物活性

描述 Istaroxime hydrochloride是Na+ / K+ ATPase的抑制剂,IC50值为0.43 μM。
靶点 Na+/K+ ATPase          
IC50 0.43 μM          

质量控制

质量控制和MSDS

批次:

化学结构

Istaroxime hydrochloride