Home Neuronal Signaling Adrenergic Receptor antagonist Esmolol For research use only.

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

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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 lnformation & 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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