Esmolol HCl

Adrenergic Receptor antagonist

Home Neuronal Signaling Adrenergic Receptor antagonist Esmolol HCl

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Esmolol (ASL8052) is a cardioselective b-blocker, used to control rapid heartbeats or abnormal heart rhythms.

Esmolol HCl Chemical Structure

Esmolol HCl Chemical Structure

Molecular Weight: 331.83

Purity & Quality Control

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

Esmolol HCl Related Products

Signaling Pathway

Adrenergic Receptor Signaling Pathways

Adrenergic Receptor Signaling Pathway

Mechanism of Action

Description Esmolol (ASL8052) is a cardioselective b-blocker, used to control rapid heartbeats or abnormal heart rhythms.
Features The suppressive effects of ONO-1101 on cardiovascular performance are less than those of Esmolol at equipotent beta-blocking doses.
Targets
beta-adrenergic receptor [1]

In vitro
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. [1]

In Vivo
In vivo Esmolol (20 mg/kg) infusion in sepsis improves oxygen utilization of myocardium and preserves myocardial function in septic rats. [2] 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%. [3] 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. [4]
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

References
  • https://pubmed.ncbi.nlm.nih.gov/7758250/
  • https://pubmed.ncbi.nlm.nih.gov/16215384/
  • https://pubmed.ncbi.nlm.nih.gov/11698317/
  • https://pubmed.ncbi.nlm.nih.gov/10413070/

Chemical Information

Molecular Weight 331.83 Formula

C16H25NO4.HCl
CAS No. 81161-17-3 SDF Download Esmolol HCl SDF
Synonyms ASL8052
Smiles CC(C)NCC(COC1=CC=C(C=C1)CCC(=O)OC)O.Cl

Storage and Stability

Storage (From the date of receipt)

In vitro
Batch:

DMSO : 66 mg/mL ( (198.89 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 66 mg/mL

Ethanol : 66 mg/mL


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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