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Amrinone

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Rating icon 很棒

纯度: 99.45%

货号 T1265Cas号 60719-84-8

别名 氨力农, Wincoram, Inocor, Inamrinone

Amrinone (Inocor) 是一种正性肌力血管扩张剂,是一种具有口服活性的,非糖苷和非儿茶酚胺的强心剂,也是一种选择性磷酸二酯酶 III (phosphodiesterase III) 抑制剂,能够防止环磷酸腺苷分解,从而增加环磷酸腺苷水平。

Amrinone
其他形式的 “Amrinone”:

Amrinone

一键复制产品信息
Rating icon 很棒

纯度: 99.45%

货号 T1265 别名 氨力农, Wincoram, Inocor, InamrinoneCas号 60719-84-8

Amrinone (Inocor) 是一种正性肌力血管扩张剂,是一种具有口服活性的,非糖苷和非儿茶酚胺的强心剂,也是一种选择性磷酸二酯酶 III (phosphodiesterase III) 抑制剂,能够防止环磷酸腺苷分解,从而增加环磷酸腺苷水平。

规格价格库存数量
50 mg
¥ 247
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100 mg
¥ 372
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200 mg
¥ 538
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500 mg
¥ 892
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1 mL x 10 mM (in DMSO)
¥ 178
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产品介绍


Amrinone AI Summary
Amrinone exhibits positive inotropic activity in both anesthetized dogs (ED50 = 0.389 mg/kg) and isolated papillary muscle of dogs, indicating an increase in myocardial contractility. It inhibits various forms of phosphodiesterase (PDE) with notable inhibitory concentrations (IC50 values) including: - PDE3 from guinea pig heart: IC50 = 50000.0 nM - PDE3 in dog aorta: IC50 = 28000.0 nM - PDE4 from the heart: IC50 = 101000.0 nM - PDE1 from the cerebral cortex: IC50 > 300000.0 nM The compound also significantly affects contractile force and frequency rate in spontaneous beating atria from Reserpine-treated guinea pigs, demonstrating an increase in both parameters at different concentrations. It has bioactivities related to hemodynamic activity, showing a dose-dependent increase in left ventricular myocardial activity in anesthetized dogs, and exhibits a significant inhibitory effect on ADP-induced platelet aggregation at higher concentrations. Additionally, Amrinone has moderate lipophilicity with a LogP value of 2.66 and shows good oral bioavailability in humans (>80%). The compound's pharmacokinetic profile indicates a high clearance rate (8.9 mL.min^-1.kg^-1) and a short half-life (T1/2 = 2.0 hr), suggesting a relatively short duration of action. On the cardiovascular side, it also demonstrates selectivity and potency against cAMP PDE III enzyme over PDE I and II, and shows significant liver metabolism markers, with effects observed on enzymes such as SGOT and SGPT. Furthermore, the compound's inhibition of human BSEP activity and its interaction with various transporters like P-gp and MRP2 hints at its complex absorption and distribution characteristics. In antiviral contexts, it shows marginal activity against SARS-CoV-2 induced cytotoxicity in Caco-2 cells, suggesting a limited antiviral potential. Overall, Amrinone demonstrates promising cardiotonic properties and PDE inhibition but requires further evaluation for its multi-target bioactivities, including its antiviral potential and liver toxicity profile..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
Amrinone (Inocor) is a positive inotropic cardiotonic (cardiotonic agent) with vasodilator properties, phosphodiesterase 3 inhibitory activity.
别名氨力农, Wincoram, Inocor, Inamrinone
化学信息
分子量187.2
分子式C10H9N3O
CAS No.60719-84-8
SmilesNC1=CC(=CNC1=O)C=2C=CN=CC2
密度1.277 g/cm3
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
溶解度信息
DMSO: 10 mg/mL (53.42 mM), Sonication is recommended.
体内实验配方
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (5.34 mM), Sonication is recommended.
请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM5.3419 mL26.7094 mL53.4188 mL267.0940 mL
5 mM1.0684 mL5.3419 mL10.6838 mL53.4188 mL
10 mM0.5342 mL2.6709 mL5.3419 mL26.7094 mL
20 mM0.2671 mL1.3355 mL2.6709 mL13.3547 mL
50 mM0.1068 mL0.5342 mL1.0684 mL5.3419 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments 比如您的给药剂量是10 mg/kg,每只动物体重20g,给药体积100 μLTargetMol | Animal experiments 一共给药动物10只,您使用的配方为5%TargetMol | reagent DMSO + 30%PEG300 + 5%Tween 80 + 60%Saline/PBS/ddH2O, 那么您的工作液浓度为2mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween80, 混匀澄清,再加 600μLSaline/PBS/ddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

方案所需的各类助溶剂如: DMSOPEG300 / PEG400Tween 80SBE-β-CD玉米油 等, 均可在TargetMol网站点击购买。
1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

剂量转换

对于不同动物的给药剂量换算,您也可以参考 更多

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