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Bisoprolol fumarate

(Synonyms: 半富马酸比索洛尔)

目录号: PC10714 纯度: ≥98%

选择性α-肾上腺素能阻断剂,Bisoprolol是β1肾上腺素受体阻断剂。

CAS No. :104344-23-2

商品编号	规格	价格	会员价
PC10714-50mg	50mg	¥357.00	请登录
PC10714-100mg	100mg	¥613.00	请登录
PC10714-250mg	250mg	¥1225.00	请登录
PC10714-500mg	500mg	¥1940.00	请登录
PC10714-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥393.00	请登录

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中文名称	Bisoprolol fumarate
中文别名	富马酸比索洛尔;比索洛尔富马酸盐;1-[4-[[2-(1-甲基乙氧基)乙氧基]甲基]-苯氧基]-3-[(1-甲基乙基)氨基]-2-丙醇富马酸盐;富马酸比索洛尔 GMP;半富马酸比索洛尔标准品;比索洛尔峰鉴别 EP标准品;比索洛尔系统适用性 EP标准品;富马酸比索洛尔 EP标准品;富马酸比索洛尔 USP标准品;富马酸比索洛尔标准品;1-4-2-(1-甲基乙氧基)乙氧基甲基-苯氧基-3-(1-甲基乙基)氨基-2-丙醇富马酸盐;比索洛尔富马酸;富马酸比索洛尔(标准品)
英文名称	Bisoprolol fumarate
英文别名	Bisoprolol Hemifumarate;1-[4-[[2-(1-METHYLETHOXY)ETHOXY]METHYL]PHENOXY]-3-[(1-METHYLETHYL)AMINO]-2-PROPANOL;(+/-)-1-[4-[[(2-(1-METHYLETHOXY)ETHOXY)METHYL]PHENOXY]-3-[(1-METHYLETHYL)AMINO]-2-PROPANOL] HEMIFUMARATE;BISOPROLOL;(+/-)-BISOPROLOL HEMIFUMARATE;CONCOR;DETENSIEL;EMCOR;EURADIAL;ISOTEN;MONOCOR;SOPROL;ZEBETA;(+-)-1-(p-((2-isopropoxyethoxy)methyl)phenoxy)-3-isopropylamino-2-propanolh;(+-)-mino)(e)-2-butenedioate(2:1)(salt);2-propanol,1-(4-((2-(1-methylethoxy)ethoxy)methyl)phenoxy)-3-((1-methylethyl)a;emd33512;emifumarate;Bisoprolol hemifumarate salt;(±)-Bisoprolol hemifumarate;2-Propanol, 1-[4-[[2-(1-methylethoxy)ethoxy]methyl]phenoxy]-3-[(1-methylethyl)amino]-, (2E)-2-butenedioate (2:1);Bisoprolol Fumarate;(+/-)-1-[4-[[2-(1-methylethoxy)ethoxy]methyl]phenoxy]-3-[(1-methyl-ethyl)amino]-2-propanol (E)-2-butenedioate;(+/-)-1-<4-(2-isopropoxyethoxymethyl)-phenoxy>-3-isopropylamino-2-propanol hemifumarate;{1-{4-[(2-isopropoxyethoxy)methyl]phenoxy}-3-(isopropylamino)propan-2-ol}2 fumarate;Seafuri;Well-bi;emifumarate bisoprolol fumarate bisoprololhemifumarate;1-[4-[[2-(1-Methylethoxy)ethoxy]methyl]phenoxy]-3-[(1-methylethyl)amino]-2-propanol hemifumarate salt;1-[4-[[2-(1-Methylethoxy)ethoxy]methyl]phenoxy]-3-[(1-methylethyl)amino]-2-propanol fumarate salt;Azopsin;Bisotate;Maintate;Bisomerck;Fondril;Emvoncor;Eurtadal;Bisobloc;Godal;Biso-Puren;Concor Plus Forte;( inverted exclamation markA)-Bisoprolol (hemifumarate);EMD 33512;DSSTox_CID_25794;DSSTox_RID_81134;DSSTox_GSID_45794;( inverted exclamation markA)-Bisoprolol hemifumarate;Zabesta;1-(4-((2-Isopropoxyethoxy)met
Cas No.	104344-23-2
分子式	C₁₈H₃₁NO₄^.₁/₂C₄H₄O₄
分子量	383.48
包装储存	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
详情描述	选择性α-肾上腺素能阻断剂,Bisoprolol是β1肾上腺素受体阻断剂。

生物活性

Bisoprolol hemifumarate is a potent, selective and orally active β1-adrenergic receptor blocker with little activity on β2-receptor. Bisoprolol hemifumarate has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research.

性状

Solid

IC50 & Target[1][2]

β adrenergic receptor

Beta-1 adrenergic receptor

体外研究(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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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).

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.
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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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.

运输条件

Room temperature or refrigerated transportation.

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)

ClinicalTrial

参考文献

[1]. Jillian G Baker, et al. The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors. Br J Pharmacol. 2005 Feb;144(3):317-22. [Information]

[2]. Jing Wang, et al. Bisoprolol, a β 1 antagonist, protects myocardial cells from ischemia-reperfusion injury via PI3K/AKT/GSK3β pathway. Fundam Clin Pharmacol. 2020 Dec;34(6):708-720. [Information]

[3]. Hong Yang, et al. Bisoprolol reverses epinephrine-mediated inhibition of cell emigration through increases in the expression of β-arrestin 2 and CCR7 and PI3K phosphorylation, in dendritic cells loaded with cholesterol. Thromb Res. 2013 Mar;131(3):230-7. [Information]

[4]. Jinhua Liu, et al. Protective Effects of Bisoprolol Against Cadmium-induced Myocardial Toxicity Through Inhibition of Oxidative Stress and NF-κΒ Signalling in Rats. J Vet Res. 2021 Oct 20;65(4):505-511. [Information]

[5]. Yajuan Ni, et al. Bisoprolol reversed small conductance calcium-activated potassium channel (SK) remodeling in a volume-overload rat model. Mol Cell Biochem. 2013 Dec;384(1-2):95-103. [Information]

溶解度数据

体外研究:

DMSO : ≥ 50 mg/mL (130.38 mM)

H₂O : 20 mg/mL (52.15 mM; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： PBS
Solubility: 100 mg/mL (260.77 mM); Clear solution; Need ultrasonic

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

Bisoprolol fumarate

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