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Enprofylline

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纯度: 98.37%

货号 T21389Cas号 41078-02-8

别名 恩丙茶碱, Enprofyllinum, Enprofilina, 3-propylxanthine, 3-n-Propylxanthine

Enprofylline (Enprofilina) 是具有选择性的 A2B 受体竞争性拮抗剂 (Ki:7 μM) ,也是磷酸二酯酶抑制剂。它可用于研究哮喘、慢性阻塞性肺疾病。

Enprofylline
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Enprofylline

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Rating icon 很棒

纯度: 98.37%

货号 T21389 别名 恩丙茶碱, Enprofyllinum, Enprofilina, 3-propylxanthine, 3-n-PropylxanthineCas号 41078-02-8

Enprofylline (Enprofilina) 是具有选择性的 A2B 受体竞争性拮抗剂 (Ki:7 μM) ,也是磷酸二酯酶抑制剂。它可用于研究哮喘、慢性阻塞性肺疾病。

规格价格库存数量
1 mg
¥ 278
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5 mg
¥ 575
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10 mg
¥ 816
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25 mg
¥ 1,470
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50 mg
¥ 2,200
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100 mg
¥ 3,170
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200 mg
¥ 4,430
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1 mL x 10 mM (in DMSO)
¥ 463
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产品介绍


Enprofylline AI Summary
Enprofylline exhibits a range of bioactivities and binding affinities across various receptors and enzymes. It shows significant affinity for the human adenosine A2B receptor (Ki = 4730.0 nM) and moderate affinity for the human adenosine A2A receptor (Ki = 32000.0 nM), rat adenosine A3 receptor (Ki = 65000.0 nM), and human adenosine A1 receptor (Ki = 44000.0 nM). It also antagonizes the binding of [3H]-N6-(phenylisopropyl) adenosine to the adenosine A1 receptor (Ki = 81000.0 nM) and the stimulation by 5'-(N-ethylcarbamoyl) adenosine of adenyl cyclase via adenosine A2 receptor (Ki = 130000.0 nM). The compound demonstrates a relaxant activity on isolated guinea pig tracheal ring chains (EC50 = 7200.0 nM) and a positive chronotropic effect on isolated guinea pig right atrium (EC15 = 18.3 µM). It shows broncho selectivity with a ratio of stimulatory activity in the right atrium to relaxant activity in tracheal muscle of 2.5 and inhibits c-AMP phosphodiesterase activity in guinea pig tracheal muscle (Ki = 43100.0 nM). In in vivo studies, Enprofylline reduces acetylcholine-induced bronchospasm in guinea pigs (ED50 = 25.7 mg·kg-1) and causes a positive chronotropic effect (ED15 = 95.1 mg·kg-1). It also exhibits moderate permeability in human skin with a log Pe value of -0.77 and demonstrates slightly lipophilic properties with a log D value of 0.27. Moreover, Enprofylline shows varying degrees of plasma protein binding across different species, with values of 60.77% in dog plasma, 67.12% in human plasma, and 78.79% in rat plasma. Additionally, it exhibits weak inhibitory effects on human BSEP (IC50 > 1000000 nM) and moderate antiviral activity against SARS-CoV-2 at 10 µM concentration. Overall, Enprofylline is a versatile bioactive compound with distinct affinity and antagonistic effects on various adenosine receptors, modest broncho-selective relaxant activity, and a range of additional pharmacological effects..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
Enprofylline (Enprofilina), a bronchodilator, acts primarily as a competitive nonselective phosphodiesterase inhibitor. Enprofylline is used in asthma, chronic obstructive pulmonary disease, and in the management of sickle cell disease, diabetic neuropathy, and cerebrovascular insufficiency.
靶点活性
A2B receptor:7 μM (Ki)
别名恩丙茶碱, Enprofyllinum, Enprofilina, 3-propylxanthine, 3-n-Propylxanthine
化学信息
分子量194.19
分子式C8H10N4O2
CAS No.41078-02-8
SmilesCCCn1c2nc[nH]c2c(=O)[nH]c1=O
密度1.367 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
H2O: Insoluble
DMSO: 60 mg/mL (308.98 mM), Sonication is recommended.
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM5.1496 mL25.7480 mL51.4960 mL257.4798 mL
5 mM1.0299 mL5.1496 mL10.2992 mL51.4960 mL
10 mM0.5150 mL2.5748 mL5.1496 mL25.7480 mL
20 mM0.2575 mL1.2874 mL2.5748 mL12.8740 mL
50 mM0.1030 mL0.5150 mL1.0299 mL5.1496 mL
100 mM0.0515 mL0.2575 mL0.5150 mL2.5748 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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