Bisoprolol hemifumarate 是一种有效的、选择性的、具有口服活性的 β1 肾上腺素受体 (β1-adrenergic receptor) 阻滞剂，对 β2 受体的活性很小。Bisoprolol hemifumarate 可用于高血压，冠状动脉疾病和稳定的心室功能障碍的研究。
| 生物活性 | Bisoprolol hemifumarate is a potent, selective and orally activeβ1-adrenergic receptorblocker with little activity on β2-receptor. Bisoprolol hemifumarate has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research[1][2]. |
| IC50& Target[1] | β adrenergic receptor | Beta-1 adrenergic receptor |
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体外研究
(In Vitro) | Bisoprolol hemifumarate (2 μM, 1 h) protects myocardial cells (H9c2) from ischemia/reperfusion (I/R) injury[2].
Bisoprolol hemifumarate (2 μM, 1 h) reduces the H/R-induced ROS production and apoptosis in H9c2 cells[2].
Bisoprolol hemifumarate (2 μM, 1 h) increases AKT and GSK3β phosphorylation in H9c2 cells[2].
Bisoprolol hemifumarate (100 μM, 24 h) reverses Epinephrine-inhibited emigration in cholesterol-loaded DCs (dendritic cell) through increasing in β-arrestin 2, CCR7 and PI3K phosphorylation[3].
Cell Viability Assay[2] | Cell Line: | H9c2 cells | | Concentration: | 0.2, 2, 20 μM | | Incubation Time: | 1 h | | Result: | Elevated the survival rates of cardiomyocytes subjected to H/R (hypoxia/reoxygenation) to 73.20%, 90.38%, 81.25% respectively. |
Cell Migration Assay[3] | Cell Line: | DCs | | Concentration: | 100 μM | | Incubation Time: | 6, 12, 24 h | | Result: | Increased the amount of migrating cells by 46.00% (6 h), 64.25% (12 h) and 55.74% (24 h). |
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体内研究
(In Vivo) | Bisoprolol hemifumarate (oral administration, 5 mg/kg, for 1 week) increases left ventricular ejection fraction (LVEF) and decreases the heart rate value[2].
Bisoprolol hemifumarate (oral gavage, 8 mg/kg, daily for four weeks) shows protective effects against Cadmium-induced myocardial toxicity in rats[4].
Bisoprolol hemifumarate (oral gavage, 1 mg/kg, daily for 6 weeks) reversessmall conductance calcium-activated potassium channel (SK) remodeling in a volume-overload rat model[5].
| Animal Model: | Ischemia/reperfusion (I/R) injury rats[2] | | Dosage: | 0.5, 5, 10 mg/kg | | Administration: | Oral administration, for 1 week, prior to 0.5 h ischemia/4 h reperfusion. | | Result: | Reduced infarct size from 44% in I/R group to 31% in treated group. |
| Animal Model: | Cadmium-induced rats[4] | | Dosage: | 2, 8 mg/kg | | Administration: | Oral gavage, daily for four weeks. | | Result: | Decreased mean arterial pressure (MAP) at 8 mg/kg.
Decreased serum biomarkers (ALT, AST) and NF-kB p65 expression and TNF-α levels (cardiac tissue samples) at 8 mg/kg. |
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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 : ≥ 50 mg/mL(130.38 mM) H2O : 20 mg/mL(52.15 mM;Need ultrasonic) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 2.6077 mL | 13.0385 mL | 26.0770 mL | | 5 mM | 0.5215 mL | 2.6077 mL | 5.2154 mL | | 10 mM | 0.2608 mL | 1.3038 mL | 2.6077 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： PBS Solubility: 100 mg/mL (260.77 mM); Clear solution; Need ultrasonic
*以上所有助溶剂都可在本网站选购。 |
