Home Neuronal Signaling Adrenergic Receptor antagonist Esmolol

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Esmolol Adrenergic Receptor antagonist

Cat.No.S5778

Esmolol is a cardioselective beta1 receptor blocker with rapid onset, a very short duration of action, and no significant intrinsic sympathomimetic or membrane stabilising activity at therapeutic dosages.
Esmolol Adrenergic Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 295.37

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S577801 DMSO]59 mg/mL]false]Water]59 mg/mL]false]Ethanol]59 mg/mL]false Purity: 99.38%
99.38

Chemical Information, Storage & Stability

Molecular Weight 295.37 Formula

C16H25NO4

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 81147-92-4 -- Storage of Stock Solutions

Synonyms N/A Smiles CC(C)NCC(COC1=CC=C(C=C1)CCC(=O)OC)O

Solubility

In vitro
Batch:

DMSO : 59 mg/mL ( (199.74 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 59 mg/mL

Ethanol : 59 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
Human β1-Receptor [1]
194 nM(Ki)
Human β2-Receptor [1]
5.8 μM(Ki)
In vitro
Esmolol acts as a pharmacochaperone: Long term exposure of cells to esmolol raised the surface levels of β1-adrenergic receptors[1].
References

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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