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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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Purity: ≥98%
Metoprolol Succinate (Toprol XL)is a potent and cardioselective β1 receptor blocker medication, which is used to treat hypertension and heart failure. In the left ventricular (LV) myocardium of dogs suffering from heart failure (HF), metoprolol reduces the rate of cardiomyocyte apoptosis. Heart failure (HF) is not necessary for metoprolol to induce the expression of Bcl-2, which in and of itself provides protection.
Targets |
β1 adrenoceptor
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ln Vitro |
Metoprolol (0-1000 μg/mL; 24-72 h) exhibits dose- and time-dependent cytotoxicity on MOLT-4 and U937 cells[3].
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ln Vivo |
Metoprolol (2.5 mg/kg/h; infusion; 11 weeks) decreases atherosclerosis and proinflammatory cytokines in ApoE-/- mice[1].
Metoprolol (15 mg/kg/q12h; i.e., 5 days) exhibits anti-viral and anti-inflammatory properties in a murine model of viral myocarditis caused by the coxsackievirus B3[2]. Metoprolol (2.5 mg/kg; intravenously; three bolus injections) inhibits myocardial apoptosis and significantly reduces the expression of activated caspase-9 protein in coronary microembolization (CME) rats[4]. |
Cell 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 reduced the viability of MOLT-4 and U937 cells at 1000 μg/mL (3740.14µM) concentration after 48 hours of incubation; similarly, after 72 hours, the viability of MOLT4 cells at ≥100 μg/ml (≥374.01µM) concentrations and U937 cells at ≥500 μg/ml (≥1870.07µM) concentrations was observed. |
Animal Protocol |
Male ApoE-/- mice
2.5 mg/kg/h Via osmotic minipumps, 11 weeks |
References | |
Additional Infomation |
Metoprolol succinate is an alcohol and a member of phenols.
Metoprolol Succinate is the succinate salt form of metoprolol, a cardioselective competitive beta-1 adrenergic receptor antagonist with antihypertensive properties and devoid of intrinsic sympathomimetic activity. Metoprolol succinate antagonizes beta 1-adrenergic receptors in the myocardium, thereby reducing the rate and force of myocardial contraction, and consequently a diminished cardiac output. This agent may also reduce the secretion of renin with subsequent reduction in levels of angiotensin II thus decreasing sympathetic activation, including vasoconstriction, aldosterone secretion.
A selective adrenergic beta-1 blocking agent that is commonly used to treat ANGINA PECTORIS; HYPERTENSION; and CARDIAC ARRHYTHMIAS. Objective: To explore the effect of metoprolol on myocardial apoptosis and caspase-9 activation after coronary microembolization (CME) in rats.[4] Methods: Forty rats were randomly divided into four groups (n=10 each): a sham operation (control) group, CME plus saline (CME) group, CME plus metoprolol (metoprolol) group and caspase-9 inhibitor Z-LEHD-FMK (ZLF) group. CME was induced by injecting 3000 polyethylene microspheres (42 μm diameter) into the left ventricle during a 10 s occlusion of the ascending aorta. Echocardiography, terminal deoxynucleotidyl transferase dUTP nick end labelling and Western blotting were used to evaluate cardiac function, apoptosis and activation of caspase-9/caspase-3, respectively, 6 h after CME.[4] Results: The echocardiographic parameters of left ventricular function were significantly decreased in the CME group compared with the control group (P<0.05); however, the metoprolol group and ZLF group showed significantly improved cardiac function compared with CME alone (P<0.05). Compared with the control group, the myocardial apoptosis rate and the levels of activated caspase-9 and -3 increased significantly in the CME group (P<0.05). Again, these effects were ameliorated by metoprolol and ZLF (P<0.05).[4] Conclusions: The present study demonstrates that metoprolol and ZLF can protect the rat myocardium during CME by inhibiting apoptosis and improving cardiac function, likely by inhibiting apoptosis/ mitochondrial apoptotic pathway. These results suggest that antiapoptotic therapies may be useful in treating CME.[4] |
Molecular Formula |
C34H56N2O10
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Molecular Weight |
652.8159
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Exact Mass |
652.39
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Elemental Analysis |
C, 62.55; H, 8.65; N, 4.29; O, 24.51
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CAS # |
98418-47-4
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Related CAS # |
Metoprolol succinate;98418-47-4;Metoprolol-d7 hydrochloride;1219798-61-4;Metoprolol tartrate;56392-17-7;Metoprolol-d7;959787-96-3;(R)-Metoprolol-d7;1292907-84-6;(S)-Metoprolol-d7;1292906-91-2;Metoprolol-d5;959786-79-9; 51384-51-1; 56392-18-8 (HCl); 80274-67-5 (fumarate); 98418-47-4 (succinate)
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PubChem CID |
62937
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Appearance |
White to off-white solid powder
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Boiling Point |
398.6ºC at 760 mmHg
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Flash Point |
194.9ºC
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LogP |
3.94
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tPSA |
176.04
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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
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InChi Key |
RGHAZVBIOOEVQX-UHFFFAOYSA-N
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InChi Code |
InChI=1S/2C15H25NO3.C4H6O4/c2*1-12(2)16-10-14(17)11-19-15-6-4-13(5-7-15)8-9-18-3;5-3(6)1-2-4(7)8/h2*4-7,12,14,16-17H,8-11H2,1-3H3;1-2H2,(H,5,6)(H,7,8)
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Chemical Name |
butanedioic acid;1-[4-(2-methoxyethyl)phenoxy]-3-(propan-2-ylamino)propan-2-ol
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Synonyms |
Metoprolol succinate; Dutoprol; Selozok; Toprol XL; Seloken-ZOK; H 93/26 succinate; Spesicor Dos; H 93/26 succinate; Toprol
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: 16.7~100 mg/mL (25.5~153.2 mM)
Water: ~100 mg/mL Ethanol: ~5 mg/mL |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (2.56 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.67 mg/mL (2.56 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.67 mg/mL (2.56 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT02123056 | Active Recruiting |
Drug: Metoprolol Drug: Matching Placebo |
Vasovagal Syncope | University of Calgary | October 2014 | Phase 4 |
NCT01608893 | Active Recruiting |
Drug: Carvedilol Drug: Metoprolol |
Atrial Fibrillation | University of Calgary | May 2012 | Not Applicable |
NCT03278509 | Active Recruiting |
Drug: Metoprolol Succinate Drug: Bisoprolol |
Acute Myocardial InfarctionST Elevation Myocardial Infarction |
Karolinska Institutet | September 11, 2017 | Phase 4 |
NCT03070184 | Active Recruiting |
Other: Exercise challenge Drug: Metoprolol Succinate ER |
Healthy Pre Hypertension |
University of Alabama at Birmingham |
April 30, 2017 | Phase 2 |
NCT05741385 | Recruiting | Drug: Caffeine Drug: Warfarin sodium Drug: Omeprazole Drug: Metoprolol |
Liver Cirrhosis | Boehringer Ingelheim | April 25, 2023 | Not Applicable |
Metoprolol dose-finding (Study I). (a) 24-hour heart rate during baseline conditions after three different doses of metoprolol compared with Control mice. Biomed Res Int . 2014:2014:548783 td> |
Metoprolol decreases atherosclerosis. Biomed Res Int . 2014:2014:548783. td> |
Photomicrographs showing the effect of metoprolol on apoptosis following coronary microembolization (original magnification ×400). Exp Clin Cardiol . 2013 Spring;18(2):161-5. td> |
Graph showing the effect of metoprolol on apoptosis following coronary microembolization (CME). Exp Clin Cardiol . 2013 Spring;18(2):161-5. td> |