Carvedilol

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Chemical Structure| 72956-09-3 同义名 : BM 14190; SKF 105517; carvedilol hydrochloride; Coropres; Querto; Kredex; Eucardic; Carvedilolum; Dilatrend; Coreg; Carvedilol (free base)
CAS号 : 72956-09-3
货号 : A361863
分子式 : C24H26N2O4
纯度 : 98%
分子量 : 406.47
MDL号 : MFCD00864692
存储条件:

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

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

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

动物实验配方:
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.
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
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 Phase 4 Withdrawn(In order to join for...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 <<
实验方案
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

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.