Nebivolol (R 065824) hydrochloride 是一种 β 受体阻滞剂,具有口服活性和高 β (1)-受体亲和力。Nebivolol hydrochloride 具有直接的血管扩张剂特性和肾上腺素能阻断特性。Nebivolol hydrochloride 可用于高血压、冠状动脉疾病、充血性心力衰竭和缺血性心脏病等多种疾病的研究。
生物活性 | Nebivolol (R 065824) hydrochloride is an orally activebeta receptorblocker and has the high beta(1)-receptor affinity.Nebivolol hydrochloride has direct vasodilator properties and adrenergic blocking characteristics. Nebivolol hydrochloride can be used for the research of kinds of diseases such as hypertension, coronary artery disease, congestive heart failure and ischemic heart disease[1][2]. |
体外研究 (In Vitro) | Nebivolol hydrochloride improves endothelial dysfunction via its strong stimulatory effects on the activity of the endothelial nitric oxide synthase and via its antioxidative properties[1]. Nebivolol hydrochloride (0.1 μM-10 μM, 1, 2, 4, 7 or 14 days) inhibits haCSMC or haEC proliferation with IC50values of ~ 6.0 μM[2]. Nebivolol hydrochloride (0.1 μM-10 μM, 24 h) induces a moderate rate of apoptosis[2]. Nebivolol hydrochloride (0.1, 1, 5,10 μM, 4 days)increases NO formation and decreases endothelin-1 secretion in HaCEs[2]
Cell Proliferation Assay[2] Cell Line: | haCSMCs (human coronary smooth muscle cells) and haECs (endothelial cells) | Concentration: | 0.1 μM-10 μM | Incubation Time: | 1, 2, 4, 7 or 14 days | Result: | Reduced proliferation in HaECs and HaCSMCs in a concentration- and time-dependent. |
Apoptosis Analysis[2] Cell Line: | haCSMCs and haECs | Concentration: | 0.1 μM-10 μM | Incubation Time: | 24 h | Result: | Induced a moderate apoptosis in concentration-dependent and showed a decrease of haCSMCs in the S-phase by 66%. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | In Vitro: DMSO : 100 mg/mL(226.30 mM;Need ultrasonic) H2O : 1.79 mg/mL(4.05 mM;ultrasonic and warming and heat to 60℃) 配制储备液 1 mM | 2.2630 mL | 11.3148 mL | 22.6296 mL | 5 mM | 0.4526 mL | 2.2630 mL | 4.5259 mL | 10 mM | 0.2263 mL | 1.1315 mL | 2.2630 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制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 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (4.71 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.71 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (4.71 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.71 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (4.71 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.71 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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