Metoprolol fumarate (CGP 2175C) 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 fumarate 具有抗炎、抗肿瘤和抗血管生成的特性。
| 生物活性 | Metoprolol fumarate (CGP 2175C) is an orally active, selectiveβ1-adrenoceptorantagonist. Metoprolol fumarate shows anti-inflammation, antitumor and anti-angiogenic properties[1][2][3]. |
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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. |
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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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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