(±)-Bisoprolol hemifumarate

SKU: orb1227073

Description

Bisoprolol is a selective type β1 adrenergic receptor blocker.(In Vitro):Bisoprolol hemifumarate (2 μM, 1 h) protects myocardial cells (H9c2) from ischemia/reperfusion (I/R) injury.Bisoprolol hemifumarate (2 μM, 1 h) reduces the H/R-induced ROS production and apoptosis in H9c2 cells.Bisoprolol hemifumarate (2 μM, 1 h) increases AKT and GSK3β phosphorylation in H9c2 cells.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.(In Vivo):Bisoprolol hemifumarate (oral administration, 5 mg/kg, for 1 week) increases left ventricular ejection fraction (LVEF) and decreases the heart rate value.Bisoprolol hemifumarate (oral gavage, 8 mg/kg, daily for four weeks) shows protective effects against Cadmium-induced myocardial toxicity in rats.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.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 104344-23-2
• MW: 383.49
• Purity: >98% (HPLC)
• Formula: C₂₀H₃₃NO₆
• SMILES: CC(C)NCC(COC1=CC=C(C=C1)COCCOC(C)C)O.CC(C)NCC(COC1=CC=C(C=C1)COCCOC(C)C)O.C(=CC(=O)O)C(=O)O
• Target: Adrenergic Receptor
• Solubility: Ethanol: 88 mg/mL (199.31 mM); Water: 88 mg/mL (199.31 mM); DMSO: 88 mg/mL (199.31 mM)

Bioactivity

• In Vivo:
  Bisoprolol hemifumarate (oral administration, 5 mg/kg, for 1 week) increases left ventricular ejection fraction (LVEF) and decreases the heart rate value. Bisoprolol hemifumarate (oral gavage, 8 mg/kg, daily for four weeks) shows protective effects against Cadmium-induced myocardial toxicity in rats. 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. Animal model: Ischemia/reperfusion (I/R) injury rats. 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. 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.
• In Vitro:
  Bisoprolol hemifumarate (2 μM, 1 h) protects myocardial cells (H9c2) from ischemia/reperfusion (I/R) injury. Bisoprolol hemifumarate (2 μM, 1 h) reduces the H/R-induced ROS production and apoptosis in H9c2 cells. Bisoprolol hemifumarate (2 μM, 1 h) increases AKT and GSK3β phosphorylation in H9c2 cells. 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. Cell Viability Assay 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 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).

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Bisoprolol hemifumarate | Zebeta | (+/-)-Bisoprolol hemifumarate | Bisobloc | Fumarate, Bisoprolol

Quick Database Links

Gene Symbol

Adrenergic Receptor