Metoprolol succinate 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 succinate 具有抗炎、抗肿瘤和抗血管生成的特性。
| 生物活性 | Metoprolol succinate is an orally active, selectiveβ1-adrenoceptorantagonist. Metoprolol succinate shows anti-inflammation, antitumor and anti-angiogenic properties[1][2][3]. |
| IC50& Target | |
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 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 中文名称 | |
| 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: H2O : ≥ 100 mg/mL(153.18 mM) DMSO : 16.67 mg/mL(25.54 mM;Need ultrasonic) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 1.5318 mL | 7.6591 mL | 15.3182 mL | | 5 mM | 0.3064 mL | 1.5318 mL | 3.0636 mL | | 10 mM | 0.1532 mL | 0.7659 mL | 1.5318 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： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 1.67 mg/mL (2.56 mM); Clear solution
此方案可获得 ≥ 1.67 mg/mL (2.56 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 16.7 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。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 1.67 mg/mL (2.56 mM); Clear solution
此方案可获得 ≥ 1.67 mg/mL (2.56 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 16.7 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。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 1.67 mg/mL (2.56 mM); Clear solution
此方案可获得 ≥ 1.67 mg/mL (2.56 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
|
