Esmolol HCl

Alias: ASL-8052; Esmolol Hydrochloride; Esmolol HCL; Brevibloc; ASL-8052; Asl 8052; ASL 8052; ASL8052; ASL 8052; Brevibloc; esmolol; esmolol hydrochloride

Cat No.:V1154 Purity: ≥98%

COA Product Data Instructions for use SDS

Esmolol HCl (Brevibloc; ASL-8052; ASL 8052), the hydrochloride salt of esmolol, is a potent and cardioselective beta-blocker used to control rapid heartbeats or abnormal heart rhythms.

Esmolol HCl Chemical Structure CAS No.: 81161-17-3
Product category: Adrenergic Receptor

This product is for research use only, not for human use. We do not sell to patients.

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Other Forms of Esmolol HCl:

Esmolol-d7 hydrochloride (esmolol d7 hydrochloride (hydrochloride))

Official Supplier of:

Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

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J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information
Biological Data

Product Description

Esmolol HCl (Brevibloc; ASL-8052; ASL 8052), the hydrochloride salt of esmolol, is a potent and cardioselective beta-blocker used to control rapid heartbeats or abnormal heart rhythms. Esmolol is an enantiomeric pair with one asymmetric center; the (+)-enantiomer is inactive and the (-)-enantiomer is active. This is similar to other P-blockers that have an oxypropranolamine nucleus. Esmolol exhibits a swift onset and offset of action, with its primary site of action being on the conduction systems of the sinus node and atrioventricular (AV) node.

Biological Activity I Assay Protocols (From Reference)

Targets

Adrenergic receptor

ln Vitro

In vitro activity: Esmolol is an enantiomeric pair with one asymmetric center; the (+)-enantiomer is inactive and the (-)-enantiomer is active. This is similar to other P-blockers that have an oxypropranolamine nucleus. Esmolol exhibits a swift onset and offset of action, with its primary site of action being on the conduction systems of the sinus node and atrioventricular (AV) node. [1]

ln Vivo

Esmolol (20 mg/kg) infusion enhances myocardial oxygen utilization and maintains myocardial function in septic rats. In rabbits, Esmolol (5 mg/kg, intravenously) causes a dose-dependent reduction in heart rate (HR), with a maximum percent reduction of 13%. In rabbits, Esmolol (5 mg/kg, intravenously) lowers mean arterial pressure (MAP) in a dose-dependent manner, with a maximum percent reduction of 38.2%. [3] In dogs, Esmolol (300 mg/kg) suppresses AV nodal conduction, increases the effective refractory period of the right ventricle and the preload of the left ventricle, and significantly lowers heart rate, rate-pressure product, left ventricular contraction, cardiac output, and relative refractory period of the right ventricle.

Animal Protocol

5 mg/kg, i.v.

Rabbits

References

[1]. Clin Pharmacokinet . 1995 Mar;28(3):190-202.

[2]. Crit Care Med . 2005 Oct;33(10):2294-301.

[3]. Can J Anaesth . 2001 Nov;48(10):985-9.

[4]. J Cardiovasc Pharmacol . 1999 Jul;34(1):70-7.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula

C16H26CLNO4

Molecular Weight

331.83

Exact Mass

331.16

Elemental Analysis

C, 57.91; H, 7.90; Cl, 10.68; N, 4.22; O, 19.29

CAS #

81161-17-3

Related CAS #

Esmolol-d7 hydrochloride; 1346598-13-7

Appearance

Solid powder

SMILES

CC(C)NCC(COC1=CC=C(C=C1)CCC(=O)OC)O.Cl

InChi Key

GEKNCWBANDDJJL-UHFFFAOYSA-N

InChi Code

InChI=1S/C16H25NO4.ClH/c1-12(2)17-10-14(18)11-21-15-7-4-13(5-8-15)6-9-16(19)20-3;/h4-5,7-8,12,14,17-18H,6,9-11H2,1-3H3;1H

Chemical Name

methyl 3-[4-[2-hydroxy-3-(propan-2-ylamino)propoxy]phenyl]propanoate;hydrochloride

Synonyms

ASL-8052; Esmolol Hydrochloride; Esmolol HCL; Brevibloc; ASL-8052; Asl 8052; ASL 8052; ASL8052; ASL 8052; Brevibloc; esmolol; esmolol hydrochloride

HS Tariff Code

2934.99.9001

Storage

Powder -20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.

Shipping Condition

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO: ~66 mg/mL (~198.9 mM)

Water: ~66 mg/mL (~198.9 mM)

Ethanol: ~66 mg/mL (~198.9 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.75 mg/mL (8.29 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.75 mg/mL (8.29 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.75 mg/mL (8.29 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

Solubility in Formulation 4: 100 mg/mL (301.36 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

(Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	3.0136 mL	15.0680 mL	30.1359 mL
	5 mM	0.6027 mL	3.0136 mL	6.0272 mL
	10 mM	0.3014 mL	1.5068 mL	3.0136 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

Molecular Weight*

Calculate Reset

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculate Reset

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

Calculate Reset

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Clinical Trial Information

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02120404	Active Recruiting	Drug: Esmolol administration	Septic Shock	Assistance Publique - Hôpitaux de Paris	April 2015	Phase 2
NCT05567822	Recruiting	Drug: Esmolol Hydrochloride Drug: normal saline	Pain, Acute Esmolol	Aretaieion University Hospital	October 1, 2022	Not Applicable
NCT05703048	Recruiting	Drug: Esmolol Esterase Drug: Dexmedetomidine	Patient's Satisfaction Depth of Anesthesia	Tanta University	December 30, 2022	Not Applicable
NCT05769868	Recruiting	Drug: Esmolol Injection [Brevibloc]	Cirrhosis Diabetes Mellitus Oncologic Disorders	Consorcio Centro de Investigación Biomédica en Red (CIBER)	April 18, 2023	Phase 3
NCT05694585	Not yet recruiting	Drug: Esmolol Drug: saline	Esmolol Stress Reaction	Xiumei Song	February 1, 2023	Phase 4

Biological Data

Panels A, B and C show representative cases of IS in the animals treated with saline (a), esmolol + milrinone (E + M) (b) and E + M in the presence of Rp-cAMPS (c). Infarcted tissue is indicated with yellow color.Cardiovasc Drugs Ther. 2011 Jun; 25(3): 223–232.

Esmolol HCl — Effects of reperfusion therapy with esmolol, milrinone or E + M on LV myocardial tissue PKA during ischemia/reperfusion.