中文名:Nebivolol hydrochloride (R-65824)
英文名:Nebivolol hydrochloride (R-65824)
英文别名:2H-1-Benzopyran-2-methanol, α,α'-[iminobis(methylene)]bis[6-fluoro-3,4-dihydro-, hydrochloride, [2R*[R*[R*(S*)]]]-(±)-
纯度:10mM in DMSO
货号:N408992
包装:1ml
Cas号:152520-56-4
存储温度:-80℃储存
产品介绍:
Information
Nebivolol HCl (R-65824) selectively inhibitsβ1-adrenoceptorwithIC50of 0.8 nM.
In vitro
Nebivolol shows high affinity and selectivity for beta 1-adrenergic receptor sites in a rabbit lung membrane preparation (Ki value = 0.9 nM and beta 2/beta 1 ratio = 50). Nebivolol displays β1-adrenoceptor selectivity with the Ki(β2)/Ki(β1) value of 40.7 judged by competition experiments to 3H-CGP 12.1777 in the presence of CGP 207.12 A (300 nM, Kiβ2) or ICI 118.551 (50 nM, Kiβ1). Nebivolol reduces cell proliferation of human coronary smooth muscle cells (haCSMCs) and endothelial cells (haECs) in a concentration- and time-dependent maner. Nebivolol treatment for 7 days causes significant reduction in cell growth of haCSMCs with IC50 of 6.1 μM, and inhibits accelerated haCSMC proliferation stimulated by growth factors PDGF-BB, bFGF, and TGFβ with IC50 values of 6.8 μM, 6.4 μM and 7.7 μM, repectively. Nebivolol treatment (10-5 M) of haCSMCs for 48 hours induces a moderate apoptosis of 23% and a decrease from 16% to 5% in the number of cells in S-phase. During Nebivolol incubation, NO formation of HaCEs increases, while endothelin-1 transcription and secretion are suppressed.
In vivo
Administratiion of Nebivolol (initially by iv within 10 minutes of reperfusion and then orally) to rats with myocardial infarction (MI) reduces myocardial apoptosis, which is mediated by regulation of NO . Nebivolol, significantly, prevents left ventricular (LV) pressure changes, reduces total and regional apoptotic cardiomyocytes. Nebivolol treatment lowers mean blood pressure (MBP) in rats with MI slightly, but not significantly.
Cell Data
cell lines:
Concentrations:Dissolved in 100% methanol and diluted with three volumes of growth medium to obtain a stock solution of 10-3 M, final concentration 10-7~10-5 M
Incubation Time:1, 2, 4, 7 and 14 days
Powder Purity:≥97%
查看阿拉丁官网此产品相关对应页面:https://www.aladdin-e.com/zh_cn/N408992.html
关键字: 2H-1-Benzopyran-2-methanol, α,α'-[iminobis(methylene)]bis[6-fluoro-3,4-dihydro-, hydrochloride, [2R*[R*[R*(S*)]]]-(±)-
上海阿拉丁生化科技股份有限公司是A股上市公司((股票代码:688179),专注于科研试剂的研发、生产和销售,已陆续建立多个工厂和研发中心。作为领军企业,阿拉丁始终坚持质量第一,连续13年被评为“最受欢迎试剂品牌”。
阿拉丁目前常备库存试剂产品品种超过7万种,SKU总数超过46万,产品线涵盖了化学试剂、生化试剂、药靶配体、蛋白质和抗体等多个领域,是国内少数化学试剂到生物试剂全面发展的国产试剂品牌,产品同步发布在我们国内外电商平台。