Esmolol
Based on 3 publication(s) in Google Scholar
Esmolol is an ultra-short-acting cardioselective β1-adrenergic blocker. Esmolol exerts its antiarrhythmic effect by activating Neurokinin 1 Receptor. Esmolol attenuates post resuscitation myocardial dysfunction. Esmolol improves diabetic wound healing by inhibiting aldose reductase and the production of advanced glycation end products and promoting fibroblast migration. Esmolol can be used to study cardiac diseases such as arrhythmias and diabetic foot ulcers.
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- CAS No.: 81147-92-4
- Formule: C16H25NO4
- Masse moléculaire:295.37
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) Esmolol
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Activité biologique
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β adrenergic receptor |
Caspase 3 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
>100 μM
Compound: Esmolol
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Antiproliferative activity against human A375 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
Antiproliferative activity against human A375 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
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[PMID: 32216987] |
| SK-MEL-28 | IC50 |
>100 μM
Compound: Esmolol
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Antiproliferative activity against human SK-MEL-28 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
Antiproliferative activity against human SK-MEL-28 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
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[PMID: 32216987] |
| SK-MEL-5 | IC50 |
>100 μM
Compound: Esmolol
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Antiproliferative activity against human SK-MEL-5 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
Antiproliferative activity against human SK-MEL-5 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
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[PMID: 32216987] |
Esmolol hydrochloride (0-1 mM) inhibits aldose reductase activity with an estimated IC50 of 150 µM, and inhibits sorbitol formation in red blood cells by 59%[1].
Esmolol hydrochloride (0.5-1 mM, 10 min) inhibits the formation of advanced glycation end products (AGEs)[1].
Esmolol hydrochloride (0.01- 1000 μM, 8-48 h) can promote the ability to migrate and has non-cytotoxic in HFF-1, Ea.hy926 and HaCaT cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HFF-1, Ea.hy926, HaCaT cells
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Concentration:0.01 μM, 0.1 μM, 1 μM, 10 μM, 50 μM, 100 μM, 500 μM, 100 μM
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Incubation Time:8 h, 14 h, 16 h, 22 h, 24 h, 42 h, 48 h
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Result:Promoted the ability to migrate, with low migration at 100 and 500 µM.
Esmolol (10 mg/kg, in 0.3 mL, i.v., once) hydrochloride shows anti-arrhythmic effect via up-egulation of NK1 receptor in permanent coronary artery occlusion (CAO) rat model[2].
Esmolol (300 μg/kg with Epinephrine 20 μg/kg, i.v., once) protects myocardial tissue and improves post-resuscitation myocardial dysfunction by reducing apoptosis in inbred wuzhishan miniature pigs[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Streptozotocin-induced (35 mg/kg/day for 5 consecutive days) diabetic hairless rats model[1]
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Dosage:7, 14, and 20%
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Administration:topical applied, twice daily
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Result:Increased the total nitrite content and NO level in wound tissue by 44% and 112% in the G14 group compared with the diabetic control group and the vehicle control group, and by 8% and 59% in the G20 group compared with the diabetic control group and the vehicle control group.
Improved collagen content, hydroxyproline levels, increased hydroxyproline levels by 22% and 44% in the G14 group, and 21% and 43% in the G20 on day 7; increased hydroxyproline levels by 6% and 13% in the G14 group, increased hydroxyproline levels by 41% and 49% in the G20 group on day 14, compared with the diabetic control and vehicle control groups.
Improved healing in G20 group and closer to normal intact diabetic skin (wounds were not completely closed on day 19) .
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Animal Model:CAO Male Sprague-Dawley rats (weighing 260 g-280 g) model[2]
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Dosage:10 mg/kg, in 0.3 mL
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Administration:i.v., once
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Result:Reduced ventricular ectopic beat (VEB) by 66%, and reduced the incidence, number, and duration of VT and VF by 66%, 92%, and 95%, respectively .
Attenuated the arrhythmogenic effects of D-SP, reducing the VEB by 45%, the morbidity rate, the episodes and the durations of VT & VF by 86%, 62% and 50% respectively, in 9-23 min following the coronary artery occlusion (CAO) (14 min-28 min after the injection of esmolol).
Increased NK1-R mRNA and protein, by 72% and 19% respectively, at 15 min after the CAO.
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Animal Model:Inbred Wuzhishan miniature pigs (12-14 months of age, 30 kg) model[3]
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Dosage:300 μg/kg with Epinephrine (HY-B0447B) 20 μg/kg
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Administration:i.v., once
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Result:Reduced the number of shocks, defibrillation energy, return of spontaneous circulation (ROSC) time and 4 h heart rate (HR), and increased the 24 h survival rate, 4-6 h CO values, 4 h mean aortic pressure (MAP) value, and 4 h left ventricular dp/dtmax.
Reduced serum cTnI, lactate concentrations and , myocardial malondialdehyde (MDA) content, increased ATPase and SOD levels.
Reduced caspase-3 proteolytic activation, mRNA levels, and TUNEL-positive cells, and attenuated apoptotic effects by upregulating Bcl-2/Bax protein levels.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 81147-92-4
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Masse moléculaire 295.37
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Formule C16H25NO4
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SMILES
O=C(OC)CCC1=CC=C(OCC(O)CNC(C)C)C=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (3)
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Journal Impact Factor
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Most Recent
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Clin Chem
Discovering Cross-Reactivity in Urine Drug Screening Immunoassays through Large-Scale Analysis of Electronic Health Records. [Abstract]2019 Dec;65(12):1522-1531. PMID: 31578215 -
EMBO Rep
2022 Jun 7;23(6):e53932. PMID: 35403787 -
J Pharm Biomed Anal
Screening method of mildronate and over 300 doping agents by reversed-phase liquid chromatography-high resolution mass spectrometry. [Abstract]2021 Feb 20:195:113870. PMID: 33453569
Pureté et documentation
Références
[2]. Wang LL, et al. Esmolol activates endogenous neurokinin activity inhibiting infarction-induced arrhythmias in rats: novel mechanisms of anti-arrhythmia. Regul Pept. 2013 Sep 10;186:116-22. [Content Brief]
[3]. Zhang Q, et al. Combination of epinephrine with esmolol attenuates post-resuscitation myocardial dysfunction in a porcine model of cardiac arrest. PLoS One. 2013 Dec 18;8(12):e82677. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Esmolol Related Classifications
HY-B1392A Related Classifications
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