Metoprolol succinate

SKU: orb1223483

Description

A selective β1 receptor blocker used in treatment of several diseases of the cardiovascular system, especially hypertension.Hypertension Approved(In Vitro):Metoprolol (0-1000 μg/mL; 24-72 h) shows cytotoxic effect on U937 and MOLT-4 cells dose and time dependently.(In Vivo):Metoprolol (2.5 mg/kg/h; infusion; 11 weeks) reduces proinflammatory cytokines and atherosclerosis in ApoE / Mice.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.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.

Key Properties

• CAS Number: 98418-47-4
• MW: 652.8159
• Purity: >98% (HPLC)
• Formula: C₃₄H₅₆N₂O₁₀
• SMILES: CC(C)NCC(COC1=CC=C(C=C1)CCOC)O.CC(C)NCC(COC1=CC=C(C=C1)CCOC)O.C(CC(=O)O)C(=O)O
• Target: Adrenergic Receptor
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  Metoprolol (2.5 mg/kg/h; infusion; 11 weeks) reduces proinflammatory cytokines and atherosclerosis in ApoE / Mice. 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. 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. Animal model: Male ApoE / mice. 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. 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.
• In Vitro:
  Metoprolol (0-1000 μg/mL; 24-72 h) shows cytotoxic effect on U937 and MOLT-4 cells dose and time dependently. Cell Cytotoxicity Assay 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 (3740.14 μM) concentration after 48 hours incubation time, significantly reduced the viability of U937 cells at ≥500 μg/ml (≥1870.07 μM) concentrations after 72 hours incubation time, and significantly decreased the viability of MOLT4 cells at ≥100 μg/ml (≥374.01 μM) concentrations after 72 hours incubation.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Adrenergic Receptor