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Olprinone

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纯度: 99.68%

货号 T5033Cas号 106730-54-5

别名 奥普力农, Loprinone

Olprinone (Loprinone) 是一种有效的磷酸二酯酶(PDE) 3抑制剂,对 PDE1,PDE2,PDE3,PDE4 的IC50分别为 150、100、0.35 和 14 μM,具有抗炎活性。它具有正性肌力和血管扩张作用,可用于心力衰竭的研究。

Olprinone
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Olprinone

一键复制产品信息
Rating icon 很棒

纯度: 99.68%

货号 T5033 别名 奥普力农, LoprinoneCas号 106730-54-5

Olprinone (Loprinone) 是一种有效的磷酸二酯酶(PDE) 3抑制剂,对 PDE1,PDE2,PDE3,PDE4 的IC50分别为 150、100、0.35 和 14 μM,具有抗炎活性。它具有正性肌力和血管扩张作用,可用于心力衰竭的研究。

规格价格库存数量
1 mg
¥ 141
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5 mg
¥ 313
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10 mg
¥ 438
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25 mg
¥ 756
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50 mg
¥ 987
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100 mg
¥ 1,450
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200 mg
¥ 2,150
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1 mL x 10 mM (in DMSO)
¥ 311
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产品介绍


Olprinone AI Summary
Olprinone exhibits a diverse range of bioactivities, being particularly notable for its antiviral and enzyme inhibitory properties. It acts as a potentiator of the human D1 dopamine receptor with a potency of 3264.1 nM and shows significant inhibition against Histone Lysine Methyltransferase G9a at 12589.3 nM. It demonstrates promising inhibitory activity against T. brucei phosphofructokinase with a potency of 756.9 nM and inhibits HP1-beta Chromodomain interactions at 5011.9 nM. In human embryonic kidney cells, Olprinone inhibits ELG1-dependent DNA repair with a potency of 18348.9 nM and exhibits dual inhibitory activity on ATXN expression with potencies of 8912.5 nM and 3162.3 nM. Furthermore, this compound inhibits the Regulator of G Protein Signaling 4 at 37685.8 nM and has demonstrated potent inhibition of Marburg virus entry into cells (446.7 nM) and Lassa virus (32.6 nM). Additionally, it shows activity against HBL1 and TMD8 cell lines with potencies of 13206.6 nM and 2956.6 nM respectively and inhibits Plasmodium falciparum proliferation at potencies ranging from 0.7 nM to 16774.4 nM. In an immunotoxin study, it shows sensitization effects with a potency of 7426.6 nM. Olprinone also possesses antiviral activity against SARS-CoV-2 (USA-WA1/2020 strain) in HRCE cells, though the activity is relatively low with a hit score of 0.1194. It exhibits selective inhibition of human HDAC6, reducing enzymatic activity by -26.79% with a commercial peptide substrate. While generally displaying high AC50 values (>30,000.0 nM) in binding affinity towards various human receptors and enzymes, it effectively inhibits human PDE3A (AC50 = 707.6 nM) and PDE4A (AC50 = 5185.5 nM) in cell-free assays..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
Olprinone (Loprinone)(Loprinone) is a selective phosphodiesterase 3 (PDE3) inhibitor.Olprinone has been reported to improve microcirculation and attenuate inflammation. Olprinone is often used to increase cardiac output after cardiopulmonary bypass (CPB).
靶点活性
PDE3:0.35 μM (IC50), PDE2:100 μM (IC50), PDE1:150 μM (IC50), PDE4:14 μM (IC50)
别名奥普力农, Loprinone
化学信息
分子量250.26
分子式C14H10N4O
CAS No.106730-54-5
SmilesCc1[nH]c(=O)c(cc1-c1ccc2nccn2c1)C#N
密度1.34g/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: 2.51 mg/mL (10.03 mM), Sonication is recommended.
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM3.9958 mL19.9792 mL39.9584 mL199.7922 mL
5 mM0.7992 mL3.9958 mL7.9917 mL39.9584 mL
10 mM0.3996 mL1.9979 mL3.9958 mL19.9792 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:
比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL, 一共给药动物10只,您使用的配方为 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline / PBS / ddH2O, 那么您的工作液浓度为2 mg/mL
母液配置方法:2 mg 药物溶于 100 μL DMSO ( 母液浓度为 20 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:100 μL DMSO 母液, 添加 400 μL PEG300 混匀澄清, 再加 50 μL Tween 80, 混匀澄清, 再加 450 μL Saline / PBS / ddH2O 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: DMSOPEG300PEG400Tween 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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