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.
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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。 |
靶点 |
|
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 | ||
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 << |
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 |
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 |