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Esmolol HCl Adrenergic Receptor antagonist

Cat.No.S4100

Esmolol (ASL8052) is a cardioselective b-blocker, used to control rapid heartbeats or abnormal heart rhythms.
Esmolol HCl Adrenergic Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 331.83

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Quality Control

Batch: S410001 DMSO]66 mg/mL]false]Water]66 mg/mL]false]Ethanol]66 mg/mL]false Purity: 99.43%
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99.43

Solubility

In vitro
Batch:

DMSO : 66 mg/mL (198.89 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 66 mg/mL

Ethanol : 66 mg/mL

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 331.83 Formula

C16H25NO4.HCl

Storage (From the date of receipt)
CAS No. 81161-17-3 Download SDF Storage of Stock Solutions

Synonyms ASL8052 Smiles CC(C)NCC(COC1=CC=C(C=C1)CCC(=O)OC)O.Cl

Mechanism of Action

Features
The suppressive effects of ONO-1101 on cardiovascular performance are less than those of Esmolol at equipotent beta-blocking doses.
Targets/IC50/Ki
beta-adrenergic receptor
In vitro
Esmolol contains one asymmetric centre and exists as an enantiomeric pair, the (-)-enantiomer is active and the (+)-enantiomer is inactive, which is analogous to other P-blockers that have an oxypropranolamine nucleus. Esmolol has a rapid onset and offset of activity, the primary site of activity of Esmolol is on sinus node and atrioventricular (AV) nodal conduction systems.
In vivo
Esmolol (20 mg/kg) infusion in sepsis improves oxygen utilization of myocardium and preserves myocardial function in septic rats. Esmolol (5 mg/kg, i.v.) produces a dose-dependent decrease in heart rate (HR) in rabbits, with the maximum percent reductions of 13%. Esmolol (5 mg/kg, i.v.) produces a dose-dependent decrease in mean arterial pressure (MAP) in rabbits, with the maximum percent reductions of 38.2%. Esmolol (300 mg/kg) significantly decreases the heart rate, rate-pressure product, left ventricular contraction, cardiac output, and relative refractory period of the right ventricle, suppresses the AV nodal conduction, and increases the effective refractory period of the right ventricle and the preload of the left ventricle in canine. Esmolol (300 mg/kg) significantly reduces the isoproterenol-induced increase in heart rate and ventricular contraction in canine.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/10413070/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06390748 Completed
Sepsis|Lymphocyte Disorder T|Immunologic Paralysis|Catecholamine; Overproduction|Beta-Blocker|Cytokine Storm|Sympathetic Nervous System Diseases
Lin Chen|Sichuan Provincial People''s Hospital
January 1 2021 Phase 2
NCT04137991 Completed
Nociceptive Pain|Goal-directed Therapy|Hemodynamic Instability|Nol-Index|Remifentanil|Cardiac Surgery|Vascular Surgery|General Anesthesia
Erasme University Hospital
October 10 2019 Not Applicable

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