货号:A361863
                
                同义名:
                    
                        
                            
                                BM 14190; SKF 105517
                            
                        
                    
                
                
                
                    
                     
                
            
Carvedilol是一种非选择性β-肾上腺素受体拮抗剂(β₁ IC₅₀=0.6 nM;β₂ IC₅₀=4.5 nM)兼α₁受体拮抗剂(IC₅₀=2.1 nM),通过多通路协同发挥心脑保护作用。Carvedilol通过抑制 cAMP/PKA通路,减轻钙超载;激活 β-arrestin2/ERK1/2通路,促进心肌细胞存活;抑制 TGF-β1/Smad3通路,阻断纤维化;调节线粒体通透性转换孔(mPTP),减少氧化损伤。
 
                                 
                                
                            

| 规格 | 价格 | 会员价 | 库存 | 数量 | |||
|---|---|---|---|---|---|---|---|
| {[ item.pr_size ]} | {[ getRatePriceInt(item.pr_rmb, 1,1) ]}{[ getRatePriceInt(item.pr_rmb_sale, 1,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]} | {[ getRatePriceInt(item.pr_rmb, 1,1) ]}{[ getRatePriceInt(item.pr_rmb,item.pr_rate,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]} | {[ getRatePriceInt(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_tag_price, item.pr_am) ]} | {[ getRatePrice(item.pr_rmb_sale, 1,1,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate,item.mem_isinteger) ]} | 现货 | 1周 咨询 | - + | 
快速发货 顺丰冷链运输,1-2 天到达
品质保证
技术支持
免费溶解
 
                        
                    
| 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 | ++++ α2A-adrenergic receptor, pKi: 8.9 α2B-adrenergic receptor, pKi: 8.9 | 97% | |||||||||||||||||
| Piribedil | ++ adrenoceptor α2A, pKi: 7.1 adrenoceptor α2C, pKi: 7.2 | 98% | |||||||||||||||||
| Prazosin HCl | ✔ | 95% | |||||||||||||||||
| Silodosin | ✔ | 98% | |||||||||||||||||
| Phenoxybenzamine HCl | ✔ | 98% | |||||||||||||||||
| Labetalol HCl | ✔ | 98+% | |||||||||||||||||
| Naftopidil | +++ α1D-adrenergic receptor, Ki: 20 nM α1A-adrenergic receptor, Ki: 3.7 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 | ✔ | 99% | |||||||||||||||||
| Doxazosin mesylate | ✔ | 99% | |||||||||||||||||
| Tolazoline HCl | ✔ | 98% | |||||||||||||||||
| Esmolol HCl | ✔ | 95% | |||||||||||||||||
| Propranolol HCl | ++ β-adrenergic receptor, IC50: 12 nM | 99% | |||||||||||||||||
| Zenidolol HCl | ++++ β2-adrenergic receptor, Ki: 0.7nM β1-adrenergic receptor, Ki: 611nM | 98% | |||||||||||||||||
| Acebutolol HCl | ✔ | 97+% | |||||||||||||||||
| Carteolol HCl | ✔ | 98+% | |||||||||||||||||
| Betaxolol | ✔ | 99% | |||||||||||||||||
| 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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 
 
 
 | 
 沪公网安备 31011702889066号
			
			沪ICP备2024050318号-1
			沪公网安备 31011702889066号
			
			沪ICP备2024050318号-1