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Metoprolol
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Metoprolol图片
CAS NO:51384-51-1
包装与价格:
包装价格(元)
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
美托洛尔
产品介绍
Metoprolol 是一种具有口服活性的、选择性的 β1-肾上腺素受体 (β1-adrenoceptor) 拮抗剂。Metoprolol 具有抗炎、抗肿瘤和抗血管生成的特性。
生物活性

Metoprolol is an orally active, selectiveβ1-adrenoceptorantagonist. Metoprolol shows anti-inflammation, antitumor and anti-angiogenic properties[1][2][3].

IC50& Target

β1 adrenoceptor

 

体外研究
(In Vitro)

Metoprolol (0-1000 μg/mL; 24-72 h) shows cytotoxic effect on U937 and MOLT-4 cells dose and time dependently[3].

Cell Cytotoxicity Assay[3]

Cell Line:U937 and MOLT-4 cells
Concentration:1, 10, 50, 100, 500 and 1000 μg/mL
Incubation Time:24, 48 and 72 h
Result:Significantly decreased the viability of U937 and MOLT-4 cells at 1000 μg/mL (3740.14μM) concentration after 48 hours incubation time, significantly reduced the viability of U937 cells at ≥500 μg/ml (≥1870.07μM) concentrations after 72 hours incubation time, and significantly decreased the viability of MOLT4 cells at ≥100 μg/ml (≥374.01μM) concentrations after 72 hours incubation.
体内研究
(In Vivo)

Metoprolol (2.5 mg/kg/h; infusion; 11 weeks) reduces proinflammatory cytokines and atherosclerosis in ApoE–/–Mice[1].
Metoprolol (15 mg/kg/q12h; i.g.; 5 days) shows anti-inflammation and anti-virus effects in murine model with coxsackievirus B3-induced viral myocarditis[2].
Metoprolol (2.5 mg/kg; i.v.; 3 bolus injections) significantly decreased activated caspase-9 protein expression and inhibits myocardial apoptosis in coronary microembolization (CME) rats[4].

Animal Model:Male ApoE–/–mice[1]
Dosage:2.5 mg/kg/h
Administration:Via osmotic minipumps, 11 weeks
Result:Significantly reduced atherosclerotic plaque area in thoracic aorta, reduced serum TNFα and the chemokine CXCL1 as well as decreasing the macrophage content in the plaques.
Animal Model:Balb/c mice, coxsackievirus B3 (CVB3) induced viral myocarditis (VMC) model[2]
Dosage:15 mg/kg/q12h
Administration:Oral gavage, 5 consecutive days
Result:Reduced pathological scores of VMC induced by CVB3 infection, protected the myocardium against viral damage by reducing serum cTn-I levels. Decreased the levels of myocardial pro-inflammatory cytokines and increase the expression of anti-inflammatory cytokine. Significantly decreased myocardial virus titers.
Clinical Trial
分子量

267.36

性状

Solid

Formula

C15H25NO3

CAS 号

51384-51-1

中文名称

美托洛尔

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : 100 mg/mL(374.03 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM3.7403 mL18.7014 mL37.4028 mL
5 mM0.7481 mL3.7403 mL7.4806 mL
10 mM0.3740 mL1.8701 mL3.7403 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 (protect from light)。-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: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.5 mg/mL (9.35 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.35 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.5 mg/mL (9.35 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.35 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在本网站选购。