GlpBio

Istaroxime hydrochloride

目录号: GC17786纯度: >99.00%同义词: ISTAROXIME盐酸盐,PST-2744 (hydrochloride);PST 2744 (hydrochloride);PST2744 (hydrochloride)
Istaroxime hydrochloride 是 Na+/K+-ATPase 抑制剂 (IC50=0.11 μM) 和肌质/内质网钙 ATPase 2 (SERCA 2) 激活剂。
Istaroxime hydrochloride
Cas No.: 374559-48-5
规格价格库存数量操作
2mg¥855.00现货
1
5mg¥1,620.00现货
1
10mg¥2,610.00现货
1
10mM (in 1mL DMSO)¥1,782.00现货
1
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文献被引

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产品描述 Description

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.

实验参考方法 Experimental Reference Method

Cell experiment: [1]

Cell lines

Guinea pig ventricular myocytes

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

4 μM, 0.5 s

Applications

Resting Ca2+ was similarly increased by istaroxime (from 61.3 to 92.4 nM). Istaroxime increased [Ca]SR-tot by 47%. Istaroxime increased the amount of Ca2+ extruded by the Na+/Ca2+ exchanger (CaNCX) during caffeine-induced transients (+130). Istaroxime shortened the time elapsing between the start of the caffeine pulse and SR Ca2+ release.
Animal experiment: [2]

Animal models

Bio TO.2 hamsters and Bio F1B hamsters

Dosage form

Oral administration, 30 mg/5 mL/kg/day

Applications

Heart function of istaroxime-treated hamsters was comparable to that of healthy animals, and had a significantly higher LVSP and both positive and negative dP/dT when compared with that of vehicle-treated animals. Coronary flow rate in hearts isolated from istaroxime-treated hamsters was higher than that from vehicle-treated Bio TO.2 animals. Besides that, Bio TO.2 hamsters treated with istaroxime had both time and frequency domain indexes of HRV, i.e. standard deviation of R-R intervals, TP, LF and HF, augmented with respect to vehicle-treated animals. Moreover , the LF/HF ratio of istaroxime-treated animals was similar to that observed in Bio F1B hamsters.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

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.

产品文档 Product Documents

Purity:>99.00%

化学性质Chemical Properties

CAS 号
374559-48-5
同义词
ISTAROXIME盐酸盐,PST-2744 (hydrochloride);PST 2744 (hydrochloride);PST2744 (hydrochloride)
化学名
(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
SMILES
CC12CCC(=NOCCN)CC1C(=O)CC3C2CCC4(C3CCC4=O)C.Cl
分子式
C21H33ClN2O3
分子量
396.95 g/mol
溶解性
DMSO : ≥ 45 mg/mL (113.36 mM); H<sub>2</sub>O : 25 mg/mL (62.98 mM; Need ultrasonic)
保存条件
4°C, sealed storage, away from moisture
General tips
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。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol