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氨力农 /Amrinone {[allProObj[0].p_purity_real_show]}

货号:A110103 同义名: Inamrinone;WIN 40,680

Amrinone is a type 3 pyridine phosphodiesterase inhibitor used in the treatment of congestive heart failure.

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Amrinone 化学结构 CAS号:60719-84-8
Amrinone 化学结构
CAS号:60719-84-8
Amrinone 3D分子结构
CAS号:60719-84-8
Amrinone 化学结构 CAS号:60719-84-8
Amrinone 3D分子结构 CAS号:60719-84-8
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Amrinone 纯度/质量文件 产品仅供科研

货号:A110103 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 PDE PDE1 PDE10A PDE2 PDE3 PDE4 PDE5 PDE6 其他靶点 纯度
Doxofylline 99+%
Deltarasin +++

PDEδ , Kd: 38 nM

99+%
7-(2,3-Dihydroxypropyl)theophylline 98%
Aminophylline +

PDE, IC50: 0.12 mM

98+%
Anagrelide HCl 99%+
Irsogladine AChR,mAChR 98%
PF-8380 +++

Autotaxin, IC50: 2.8 nM

99%+
Dipyridamole 98%
Balipodect ++++

PDE10A, IC50: 0.3 nM

99%+
PF-2545920 ++++

PDE10A, IC50: 0.37 nM

97%
Luteolin +

PDE1, Ki: 15.0 μM

++

PDE2, Ki: 6.4 μM

+

PDE3, Ki: 13.9 μM

+

PDE4, Ki: 11.1 μM

+

PDE5, Ki: 9.5 μM

98%
Milrinone ++

PDE2, IC50: 5.2 μM

++

PDE3, IC50: 2.1 μM

ATPase 98%
Pimobendan ++

PDE3, IC50: 0.32 μM

98%
Cilostazol ++

PDE3, IC50: 0.2 μM

98%
Fenspiride HCl +

PDE3, pIC50: 3.44

+

PDE4, pIC50: 4.16

98%
(S)-(+)-Rolipram ++

PDE4, IC50: 0.75 μM

98%
Apremilast +++

PDE4, IC50: 74 nM

98%
GSK256066 ++++

PDE4B, IC50: 3.2 pM

98+%
Roflumilast ++++

PDE4A4, IC50: 4.3 nM

PDE4A1, IC50: 0.7 nM

99%
Rolipram +++

PDE4B, IC50: 130 nM

99%+
Cilomilast +++

LPDE4, IC50: 100 nM

HPDE4, IC50: 120 nM

98+%
Avanafil ++++

PDE5, IC50: 1 nM

98%
Vardenafil HCl Trihydrate ++++

PDE5, IC50: 0.7 nM

98%
Tadalafil ++++

PDE5, IC50: 1.8 nM

98%
Icariin ++

PDE5, IC50: 0.432 μM

98%
Sildenafil +++

PDE6, IC50: 33 nM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Amrinone 生物活性

描述 Amrinone is a type 3 pyridine phosphodiesterase inhibitor used in the treatment of congestive heart failure. Amrinone increases cyclic adenosine monophosphate by preventing its breakdown[3]. Amrinone is administered subcutaneously to rats at a dose of 10 mg/kg/day for 14 days, significant reduction of neointimal thickness was noted. Amrinone produced a dose-dependent inhibition of ADP-induced rat platelet aggregation in vitro as well as ex vivo in rats. The proliferation of human aortic smooth muscle cells in culture stimulated with FBS or PDGF was also inhibited by amrinone[4]. Amrinone produced positive inotropic and lusitropic effects in both conscious and anesthetized dogs with autonomic nervous system blockade[5]. Amrinone caused enhancement of right ventricular contractility and afterload reduction[6]. Augmentation of myocardial contraction by amrinone in patients with chronic coronary artery disease and severe baseline left ventricular dysfunction predicts improvement in left ventricular ejection fraction after coronary artery bypass graft surgery[7].

Amrinone 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02174029 - Completed - Canada, British Columbia ... 展开 >> Royal Columbian Hospital New Westminster, British Columbia, Canada, V3L 3W7 收起 <<
NCT00060840 - Completed - -
NCT00060840 Congestive Heart Failure Phase 2 Completed - United States, New Jersey ... 展开 >> Newark Beth Isreal Medical Center Newark, New Jersey, United States, 07112 United States, North Carolina Duke University Medical Center Durham, North Carolina, United States, 27710 United States, Ohio University of Cincinnati Cincinnati, Ohio, United States, 45219 Cleveland Clinic Foundation Cleveland, Ohio, United States, 44195 United States, Pennsylvania Allegheny General Hospital Pittsburgh, Pennsylvania, United States, 15212 United States, Texas Baylor University Medical Center Dallas, Texas, United States, 75226 University of Texas/St. Paul Medical Center Dallas, Texas, United States, 75390 Texas Heart Institute Houston, Texas, United States, 20345 Germany Herz-und Diabeteszentrum Nordrhein-Westfalen Gergstrab, Bad Oeynhausen, Germany, 32545 Deutsches Herfzzentrum Berlin Augustenburger Platz, Berlin, Germany, 13353 United Kingdom Harefield Hospital Harefield, Middlesex, United Kingdom, UB96JH 收起 <<

Amrinone 参考文献

[1]Asif M. Phosphodiesterase-III Inhibitors Amrinone and Milrinone on Epilepsy and Cardiovascular Activities. N Am J Med Sci. 2012 Oct;4(10):499-502.

[2]Xiong W, Ferrier GR, Howlett SE. Diminished inotropic response to amrinone in ventricular myocytes from myopathic hamsters is linked to depression of high-gain Ca2+-induced Ca2+ release. J Pharmacol Exp Ther. 2004 Aug;310(2):761-73.

[3]Ichioka S, Nakatsuka T, Ohura N, Sato Y, Harii K. Clinical use of amrinone (a selective phosphodiesterase III inhibitor) in reconstructive surgery. Plast Reconstr Surg. 2001 Dec;108(7):1931-7

[4]Hachisu M, Nomura M, Fujishima K. [Effects of amrinone, an inhibitor of c-AMP-specific phosphodiesterases, on neointimal hyperplasia after balloon injury in rats]. Nihon Yakurigaku Zasshi. 1998 Oct;112(4):267-74. Japanese

[5]Pagel PS, Hettrick DA, Warltier DC. Amrinone enhances myocardial contractility and improves left ventricular diastolic function in conscious and anesthetized chronically instrumented dogs. Anesthesiology. 1993 Oct;79(4):753-65

[6]Ochiai Y, Morita S, Tanoue Y, Kawachi Y, Tominaga R, Yasui H. Effects of amrinone, a phosphodiesterase inhibitor, on right ventricular/arterial coupling immediately after cardiac operations. J Thorac Cardiovasc Surg. 1998 Jul;116(1):139-47

[7]Perez-Baliño NA, Masoli OH, Meretta AH, Rodriguez A, Cragnolino DE, Perrone S, Boullon F, Mele E, Palacios I, Brown KA. Amrinone stimulation test: ability to predict improvement in left ventricular ejection fraction after coronary bypass surgery in patients with poor baseline left ventricular function. J Am Coll Cardiol. 1996 Nov 15;28(6):1488-92

Amrinone 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

5.34mL

1.07mL

0.53mL

26.71mL

5.34mL

2.67mL

53.42mL

10.68mL

5.34mL

Amrinone 技术信息

CAS号60719-84-8
分子式C10H9N3O
分子量 187.198
别名 Inamrinone;WIN 40,680
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Sealed in dry,2-8°C

溶解度

DMSO: 16 mg/mL(85.47 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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