(±)-Bisoprolol hemifumarate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

比索洛尔是一种选择性 β1 型肾上腺素受体阻滞剂。

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.

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 hResult: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).

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.

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

Endocrinology/Hormones

Adrenergic Receptor

β1-adrenergic receptor

Inflammation/Immunology

——

104344-23-2

383.49

C20H33NO6

>98% (HPLC)

Ethanol: 88 mg/mL (199.31 mM); Water: 88 mg/mL (199.31 mM); DMSO: 88 mg/mL (199.31 mM)

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

(E)-but-2-enedioic acid;1-(propan-2-ylamino)-3-[4-(2-propan-2-yloxyethoxymethyl)phenoxy]propan-2-ol

(-20℃)

With Ice Pack

≥ 2 years