Esmolol

Catalog No.S5778 Batch:S577801

Technical Data

Formula	C₁₆H₂₅NO₄
Molecular Weight	295.37	CAS No.	81147-92-4
Solubility (25°C)*	In vitro	DMSO	59 mg/mL (199.74 mM)
		Water	59 mg/mL (199.74 mM)
		Ethanol	59 mg/mL (199.74 mM)
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

Esmolol acts as a pharmacochaperone: Long term exposure of cells to esmolol raised the surface levels of β1-adrenergic receptors^[1].

Protocol (from reference)

Cell Assay:^{^[1]}	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.

Cell Assay:^{^[1]}

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.

References

[1] Nasrollahi-Shirazi S, et al. J Pharmacol Exp Ther. 2016, 359(1):73-81.

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SHIPPING AND STORAGE
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