aladdin 阿拉丁 N408992 Nebivolol hydrochloride (R-65824) 152520-56-4 10mM in DMSO

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 (K_i value = 0.9 nM and beta 2/beta 1 ratio = 50). Nebivolol displays β1-adrenoceptor selectivity with the K_i(β2)/K_i(β1) value of 40.7 judged by competition experiments to ³H-CGP 12.1777 in the presence of CGP 207.12 A (300 nM, K_iβ2) or ICI 118.551 (50 nM, K_iβ1). 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%

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