Nebivolol hydrochloride是第三代β1肾上腺素受体选择性拮抗剂，Nebivolol hydrochloride通过高选择性阻断β1受体并激活一氧化氮（NO）介导的血管扩张双重机制发挥降压作用，同时对外周血管阻力、代谢及性功能影响。
Cas No.:152520-56-4
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
Nebivolol hydrochloride is a third-generation, selective β1-adrenergic receptor antagonist. Nebivolol hydrochloride exerts its antihypertensive effect through a dual mechanism involving highly selective β1-blockade and activation of nitric oxide (NO)-mediated vasodilation, while having minimal impact on peripheral vascular resistance, metabolism, and sexual function[1-2]. Nebivolol hydrochloride is used in research related to hypertension, chronic heart failure, and angina pectoris[3-4].
In vitro, Nebivolol hydrochloride (0–50µM) was applied to oral squamous cell carcinoma (OSCC) cells for 24 hours. Nebivolol hydrochloride activated the endoplasmic reticulum stress signaling pathway by inducing iNOS expression, leading to G0/G1 cell cycle arrest and growth inhibition. Nebivolol hydrochloride also caused mitochondrial dysfunction, increased reactive oxygen species (ROS) levels, and induced apoptosis[5]. In melanoma cells (A2058 and B16) treated with Nebivolol hydrochloride (5–10µM) for 24 hours, Nebivolol hydrochloride reduced cAMP levels, which resulted in G0/G1 cell cycle arrest. Nebivolol hydrochloride triggered loss of mitochondrial membrane potential (ΔΨm), accumulation of ROS, activation of the mitochondrial apoptosis pathway, and suppression of migration and invasion capabilities[6].
In vivo, Nebivolol hydrochloride (15mg/kg; single dose) was administered intraperitoneally to mice with maximal electroshock-induced seizures in combination with other antiepileptic drugs. Nebivolol hydrochloride significantly attenuated the anticonvulsant effects of carbamazepine and phenobarbital[7]. Nebivolol hydrochloride (2.0μmol/kg/day) was administered via diet to apolipoprotein E (apoE) knockout mice for 4 months starting at 8 weeks of age. Nebivolol hydrochloride significantly reduced atherosclerotic plaque area in both the aortic root and the entire aorta, without affecting plasma cholesterol or triglyceride levels[8].
References:
[1] Cockcroft J. Nebivolol: a review. Expert Opin Pharmacother. 2004 Apr;5(4):893-9.
[2] de Boer RA, Voors AA, van Veldhuisen DJ. Nebivolol: third-generation beta-blockade. Expert Opin Pharmacother. 2007 Jul;8(10):1539-50.
[3] Battise D, Boland CL, Nuzum DS. Nebivolol/Valsartan: A Novel Antihypertensive Fixed-Dose Combination Tablet. Ann Pharmacother. 2019 Apr;53(4):402-412.
[4] Gao Y, Vanhoutte PM. Nebivolol: an endothelium-friendly selective β1-adrenoceptor blocker. J Cardiovasc Pharmacol. 2012 Jan;59(1):16-21.
[5] Chen Q, Jiang H, Wang Z, et al. Adrenergic Blockade by Nebivolol to Suppress Oral Squamous Cell Carcinoma Growth via Endoplasmic Reticulum Stress and Mitochondria Dysfunction. Front Pharmacol. 2021 Aug 12;12:691998.
[6] Yang S, Li Z, Yi J, et al. Nebivolol, an antihypertensive agent, has new application in inhibiting melanoma. Anticancer Drugs. 2024 Jul 1;35(6):512-524.
[7] Borowicz-Reutt KK, Banach M, Rudkowska M. Nebivolol attenuates the anticonvulsant action of carbamazepine and phenobarbital against the maximal electroshock-induced seizures in mice. Pharmacol Rep. 2020 Feb;72(1):80-86.
[8] Kus K, Gajda M, Pyka-Fosciak G, et al. The effect of nebivolol on atherogenesis in apoE-knockout mice. J Physiol Pharmacol. 2009 Dec;60(4):163-5.
Nebivolol hydrochloride是第三代β1肾上腺素受体选择性拮抗剂，Nebivolol hydrochloride通过高选择性阻断β1受体并激活一氧化氮（NO）介导的血管扩张双重机制发挥降压作用，同时对外周血管阻力、代谢及性功能影响[1-2]。Nebivolol hydrochloride可用于高血压、慢性心力衰竭和心绞痛的相关研究[3-4]。
在体外，Nebivolol hydrochloride（0-50μM）处理口腔鳞状细胞癌（OSCC）细胞24小时，Nebivolol hydrochloride通过诱导iNOS表达激活内质网应激信号通路，导致细胞周期G0/G1期阻滞和生长抑制。Nebivolol hydrochloride可引起线粒体功能障碍，增加活性氧（ROS）水平，诱导细胞凋亡[5]。Nebivolol hydrochloride（5-10μM）处理黑色素瘤细胞（A2058和B16）24小时，Nebivolol通过降低cAMP水平诱导G0/G1期细胞周期阻滞。Nebivolol hydrochloride可引起线粒体膜电位（ΔΨm）丧失和ROS积累，激活线粒体途径凋亡，并抑制迁移侵袭能力[6]。
在体内，Nebivolol hydrochloride（15mg/kg）腹腔注射处理最大电休克诱导癫痫模型小鼠（单次给药，与抗癫痫药物联用），Nebivolol hydrochloride显著减弱卡马西平和苯巴比妥的抗惊厥作用[7]。Nebivolol hydrochloride（2.0μmol/kg/day）经饲料给药处理apoE基因敲除小鼠（从8周龄开始，持续4个月），Nebivolol hydrochloride显著减轻主动脉根部和整体主动脉的动脉粥样硬化斑块面积，且不影响血浆胆固醇和甘油三酯水平[8]。
| Cell experiment [1]: | |
Cell lines | HSC-3 and HN12 cells (human oral squamous cell carcinoma cell lines) |
Preparation Method | Cells were cultured in high-glucose DMEM supplemented with 10% fetal bovine serum and 1% antibiotics at 37°C under 5% CO₂. Cells were treated with Nebivolol hydrochloride at concentrations of 0–50µM for 24 hours. |
Reaction Conditions | 0–50µM; 24 hours. |
Applications | Nebivolol hydrochloride significantly induced endoplasmic reticulum (ER) stress by upregulating iNOS expression, activating the PERK-eIF2α-ATF4-CHOP signaling pathway, and triggering integrated stress response (ISR) gene expression. Nebivolol hydrochloride concurrently caused mitochondrial dysfunction, characterized by reduced complex I activity, impaired electron transport chain function, and fragmented mitochondrial morphology. These effects led to increased reactive oxygen species (ROS) production, G0/G1 cell cycle arrest, and caspase-3-mediated apoptosis. Nebivolol hydrochloride also inhibited colony formation and cell viability in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Female apolipoprotein E (apoE)-knockout mice on C57BL/6J background |
Preparation Method | Mice were fed a standard chow diet mixed with a racemic mixture of D- and L-Nebivolol hydrochloride at a dose of 2.0μmol/kg/day for 4 months, starting at 8 weeks of age. Mice were sacrificed at 6 months of age under anesthesia for analysis. |
Dosage form | 2.0μmol/kg/day; oral administration; chronic treatment (4 months). |
Applications | Nebivolol hydrochloride significantly attenuated atherogenesis, reducing atherosclerotic lesion area and aortic roots. The anti-atherogenic effect was independent of changes in plasma cholesterol or triglyceride levels. Nebivolol hydrochloride likely exerted protective action by enhancing endothelial nitric oxide (NO) bioavailability, inhibiting NADPH oxidase activity, reducing oxidative stress, and suppressing inflammatory adhesion molecules and prothrombotic factors. |
References: | |
| Cas No. | 152520-56-4 | SDF | |
| 别名 | 盐酸奈必洛尔; R 065824 hydrochloride | ||
| 化学名 | (1S)-1-[(2S)-6-fluoro-3,4-dihydro-2H-chromen-2-yl]-2-[[(2S)-2-[(2R)-6-fluoro-3,4-dihydro-2H-chromen-2-yl]-2-hydroxyethyl]amino]ethanol;hydrochloride | ||
| Canonical SMILES | C1CC2=C(C=CC(=C2)F)OC1C(CNCC(C3CCC4=C(O3)C=CC(=C4)F)O)O.Cl | ||
| 分子式 | C22H26ClF2NO4 | 分子量 | 441.9 |
| 溶解度 | ≥ 22.1mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 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°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.263 mL | 11.3148 mL | 22.6296 mL |
| 5 mM | 452.6 μL | 2.263 mL | 4.5259 mL |
| 10 mM | 226.3 μL | 1.1315 mL | 2.263 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet