Esmolol

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 Chemical Structure

Esmolol Chemical Structure

CAS: 81147-92-4

Purity & Quality Control

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

Esmolol Related Products

Choose Selective Adrenergic Receptor Inhibitors

Biological Activity

Description 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.
Targets
Human β1-Receptor [1] Human β2-Receptor [1]
194 nM(Ki) 5.8 μM(Ki)
In vitro
In vitro Esmolol acts as a pharmacochaperone: Long term exposure of cells to esmolol raised the surface levels of β1-adrenergic receptors[1].
Cell Research Cell lines HEK293 cells expressing human β1- and β2-adrenergic receptors
Concentrations 1 μM
Incubation Time 40 min
Method

Cells are seeded into 6-cm dishes in DMEM containing 10% FCS, allowed to adhere for 8 hours, and then rendered quiescent by serum starvation for 16 hours. Cells are subsequently stimulated by addition of medium containing or lacking 1 μM esmolol, 1 μM landiolol, or 1 μM isoproterenol (as a positive control). Cells are maintained at 37°C for up to 40 minutes, the incubation is terminated by rapid rinsing with ice-cold PBS. Thereafter, the dish is immediately immersed in liquid nitrogen. After rapid thawing, cells were disrupted by addition of 80 μl of lysis buffer, 1% Nonidet P-40, 0.1% SDS, 250 IU/ml aprotinin, and 40 μg/ml leupeptin. The cellular debris was removed by centrifugation at 10,000g for 10 minutes, and the total protein content was measured photometrically using bicinchoninic acid.

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
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
NCT02455440 Completed
Cerebral Arterial Disease|Cerebral Aneurysm
George Papanicolaou Hospital
March 2014 Phase 3

Chemical Information & Solubility

Molecular Weight 295.37 Formula

C16H25NO4

CAS No. 81147-92-4 SDF --
Smiles CC(C)NCC(COC1=CC=C(C=C1)CCC(=O)OC)O
Storage (From the date of receipt) 3 years -20°C powder

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


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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.

Handling Instructions

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