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Carvedilol/卡维地洛 {[allProObj[0].p_purity_real_show]}

货号:A361863 同义名: BM 14190; SKF 105517

Carvedilol can block β-1 and β-2 adrenergic receptors as well as the α-1 adrenergic receptors, indicated in the treatment of mild to moderate congestive heart failure.

Carvedilol/卡维地洛 化学结构 CAS号:72956-09-3
Carvedilol/卡维地洛 化学结构
CAS号:72956-09-3
Carvedilol/卡维地洛 3D分子结构
CAS号:72956-09-3
Carvedilol/卡维地洛 化学结构 CAS号:72956-09-3
Carvedilol/卡维地洛 3D分子结构 CAS号:72956-09-3
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Carvedilol/卡维地洛 纯度/质量文件 产品仅供科研

货号:A361863 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Adrenergic Receptor α-adrenergic receptor β-adrenergic receptor 其他靶点 纯度
Ivabradine HCl 98%
Maprotiline HCl 98%
Cisatracurium besylate 96%
Yohimbine HCI 99+%
BMY 7378 ++

α1D-adrenoceptor, pKi: 5.1

α2C-adrenoceptor, pKi: 6.54

+

β1-adrenoceptor, pIC50: 5.1

97%
Asenapine maleate ++++

α2B-adrenergic receptor, pKi: 8.9

α2A-adrenergic receptor, pKi: 8.9

97%
Piribedil ++

adrenoceptor α2C, pKi: 7.2

adrenoceptor α2A, pKi: 7.1

98%
Prazosin HCl 95%
Silodosin 98%
Phenoxybenzamine HCl 98%
Labetalol HCl 98+%
Naftopidil +++

α1A-adrenergic receptor, Ki: 3.7 nM

α1D-adrenergic receptor, Ki: 20 nM

98%
Naftopidil 2HCl +

α1-adrenergic receptor, IC50: 0.2 μM

99%
Alfuzosin HCl 98%
Terazosin HCl 99%
Atipamezole 95%
Phentolamine methanesulfonate salt 99%
Carvedilol 98%
Doxazosin mesylate 99%
Tolazoline HCl 98%
Esmolol HCl 95%
Propranolol HCl ++

β-adrenergic receptor, IC50: 12 nM

98%
Zenidolol HCl ++++

β2-adrenergic receptor, Ki: 0.7nM

β1-adrenergic receptor, Ki: 611nM

98%
Acebutolol HCl 97+%
Carteolol HCl 98+%
Betaxolol 95%
Betaxolol HCl +

β1-adrenergic receptor, IC50: 6 μM

97%
Bisoprolol 97%
Sotalol HCl 95+%
Nebivolol HCl +++

β1-adrenoceptor, IC50: 0.8 nM

99%
Metoprolol 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。

Carvedilol/卡维地洛 生物活性

靶点
  • α-adrenergic receptor

描述 Carvedilol is a non-selective beta blocker/alpha-1 blocker with an IC50 of 3.8 μM for inhibition of LDL oxidation.

Carvedilol/卡维地洛 细胞研究

细胞系 浓度 检测类型 检测时间 活性说明 数据源
BESM cells Cytotoxicity assay 88 h Cytotoxicity against BESM cells after 88 hrs by HTS assay, EC50=31 μM 20547819
CHO cells Function assay Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique, IC50=10.4713 μM 18448342
HEK293 cells Function assay 3 mins Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay, IC50=7.5 μM 23241029
ScN2a-cl3 cells Cytotoxicity assay Cytotoxicity against mouse dividing ScN2a-cl3 cells assessed as cell viability after 5 days by calcein-AM staining-based fluorescence assay, LC50=6.1 μM 24183589

Carvedilol/卡维地洛 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
NCT00374465 Dilated Cardiomyopathy Phase 4 Unknown - Poland ... 展开 >> Silesian Centre for Heart Disease, 3rd Department of Cardiology Recruiting Zabrze, Szpitalna 2 st., Poland, 41800 Principal Investigator: Romuald Wojnicz, MD, PhD          Sub-Investigator: Ewa N Kozielska, MD, PhD          Sub-Investigator: Jolanta Nowak, MD          Sub-Investigator: Krzysztof Wilczek, MD          Sub-Investigator: Celina Wojciechowska, MD          Sub-Investigator: Bozena Szygula, MD 收起 <<
NCT01009918 Breast Cancer ... 展开 >> Cardiac Toxicity 收起 << Phase 2 Active, not recruiting November 2018 -
NCT00384566 Heart Failure ... 展开 >> Chronic Obstructive Airway Disease 收起 << Phase 4 Withdrawn(In order to join for... 展开 >>ces with another study already running which aims to answer the same question.) 收起 << - Australia, Victoria ... 展开 >> Alfred Hospital Melbourne, Victoria, Australia, 3004 收起 <<

Carvedilol/卡维地洛 参考文献

[1]Chen J, Huang C, et al. The effects of carvedilol on cardiac structural remodeling: the role of endogenous nitric oxide in the activity of carvedilol. Mol Med Rep. 2013 Apr;7(4):1155-8.

[2]Stafylas PC, Sarafidis PA. Carvedilol in hypertension treatment. Vasc Health Risk Manag. 2008;4(1):23-30.

Carvedilol/卡维地洛 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.46mL

0.49mL

0.25mL

12.30mL

2.46mL

1.23mL

24.60mL

4.92mL

2.46mL

Carvedilol/卡维地洛 技术信息

CAS号72956-09-3
分子式C24H26N2O4
分子量 406.47
SMILES Code OC(CNCCOC1=CC=CC=C1OC)COC2=CC=CC(N3)=C2C4=C3C=CC=C4
MDL No. MFCD00864692
别名 BM 14190; SKF 105517; carvedilol hydrochloride; Coropres; Querto; Kredex; Eucardic; Carvedilolum; Dilatrend; Coreg; Carvedilol (free base)
运输蓝冰
InChI Key OGHNVEJMJSYVRP-UHFFFAOYSA-N
Pubchem ID 2585
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C

溶解方案

DMSO: 105 mg/mL(258.32 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

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