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Bucindolol

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纯度: 99.9%

货号 T10631Cas号 71119-11-4

别名 布新洛尔, MJ 131051, MJ 13105, BMY 13105

Bucindolol (BMY 13105) 是一种新型有效的 β1 肾上腺素能受体 (β1-adrenergic receptor) 阻滞剂,可介导血管舒张,可用于研究慢性心力衰竭。

Bucindolol

Bucindolol

一键复制产品信息
Rating icon 很棒

纯度: 99.9%

货号 T10631 别名 布新洛尔, MJ 131051, MJ 13105, BMY 13105Cas号 71119-11-4

Bucindolol (BMY 13105) 是一种新型有效的 β1 肾上腺素能受体 (β1-adrenergic receptor) 阻滞剂,可介导血管舒张,可用于研究慢性心力衰竭。

规格价格库存数量
1 mg
¥ 397
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2 mg
¥ 591
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5 mg
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产品介绍


Bucindolol AI Summary
Bucindolol exhibits a wide range of bioactivities across various biological systems. It acts as a beta-adrenergic receptor blocker in normotensive rats, achieving 71.0% inhibition at 2 mg/kg, and demonstrates intrinsic sympathomimetic activity with 77.0 beats per minute in reserpinized rats. Additionally, it shows antihypertensive effects in spontaneously hypertensive rats with a 45.0 mmHg reduction in blood pressure following peroral administration and possesses vasodilator activity in ganglion-blocked rats, leading to a 26.0% decrease in mean arterial blood pressure at 3 mg/kg intravenously. Bucindolol is a potent inhibitor of the enzyme Cytochrome P450 2D6 (CYP2D6), with an IC50 value of 50.0 nM after 45 minutes of incubation. It also significantly inhibits the uptake of 4-(4-(dimethylamino)styryl)-N-methylpyridinium via human OCT1 in HEK293 cells, with an IC50 of 27,200.0 nM and 84.6% inhibition at a concentration of 100 µM. The compound shows diverse bioactivity in various other assays, including inhibition of the Menin-MLL interaction in MLL-related leukemias, GCN5L2 inhibition, delayed death inhibition of the malarial parasite plastid, and Schwann cell viability assays. Additionally, it induces DNA re-replication in SW480 colon adenocarcinoma cells, inhibits human tyrosyl-DNA phosphodiesterase 1 (TDP1), blocks viral entries, including Lassa Virus, Marburg Virus, Ebola Virus, and SARS-CoV-2, with an IC50 ranging from 16,982.44 nM to 17,000.0 nM for SARS-CoV-2. The compound also inhibits insulin secretion from INS-1E cells at different glucose concentrations, with varying potencies in the nanomolar and micromolar ranges. Lastly, Bucindolol exhibits antiviral activity against SARS-CoV-2 in VERO-E6 cells, demonstrating an IC50 range of 16,982.44 nM to 17,000.0 nM and a CC50 value of 30,900.0 nM, indicating both its potency and certain cytotoxicity to VERO-E6 cells..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
Bucindolol (BMY 13105) is a novel and potent β1-adrenergic receptor blocker that mediates vasodilation and can be used to study chronic heart failure.
别名布新洛尔, MJ 131051, MJ 13105, BMY 13105
化学信息
分子量363.45
分子式C22H25N3O2
CAS No.71119-11-4
SmilesCC(C)(Cc1c[nH]c2ccccc12)NCC(O)COc1ccccc1C#N
密度1.31g/cm3
储存&溶解度
存储store at low temperature | 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: 80 mg/mL (220.11 mM), Sonication is recommended.
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM2.7514 mL13.7571 mL27.5141 mL137.5705 mL
5 mM0.5503 mL2.7514 mL5.5028 mL27.5141 mL
10 mM0.2751 mL1.3757 mL2.7514 mL13.7571 mL
20 mM0.1376 mL0.6879 mL1.3757 mL6.8785 mL
50 mM0.0550 mL0.2751 mL0.5503 mL2.7514 mL
100 mM0.0275 mL0.1376 mL0.2751 mL1.3757 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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