A β1-AR antagonist
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Active Metabolite(s)
35295Esmolol Acid (hydrochloride)
Labeled Version(s)
30727Esmolol-d7 (hydrochloride)
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Esmolol (hydrochloride)

Item No. 22581

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[2-hydroxy-3-[(1-methylethyl)amino]propoxy]-benzenepropanoic acid, methyl ester, monohydrochloride
CAS Number
81161-17-3
Synonyms
  • ASL 8052
Molecular Formula
C16H25NO4 • HCl
Formula Weight
331.8
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMSO: 25 mg/mlEthanol: 25 mg/mlPBS (pH 7.2): 10 mg/ml
λmax
224, 276, 283 nm
SMILES
CC(C)NCC(O)COC1=CC=C(CCC(OC)=O)C=C1.Cl
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
InChi Key
GEKNCWBANDDJJL-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    10 mg

    $36

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    50 mg

    $128

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    100 mg

    $236

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    500 mg

    $1,003

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    Product Description

    Esmolol is a β1-adrenergic receptor (β1-AR) antagonist.1 It binds to β1-ARs (Kd = 100 nM in isolated cardiac myocytes) and is 34-fold selective for β1- over β2-ARs.1,2 Esmolol also inhibits L-type Ca2+ currents (ICa.L) and the fast Na+ current (INa) in rat cardiac myocytes (IC50s = 50 and 169 μM, respectively), which results in complete ventricular arrest at concentrations greater than or equal to 1 mM.1 Formulations containing esmolol have been used in the treatment of cardiac arrhythmias, postoperative hypertension, and acute ischemic heart disease, as well as to minimize myocardial contraction during cardiac surgery and attenuate the adrenergic response associated with tracheal intubation.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Fallouh, H.B., Bardswell, S.C., McLatchie, L.M., et al. Esmolol cardioplegia: The cellular mechanism of diastolic arrest. Cardiovasc. Res. 87(3), 552-560 (2010).

    2. Jahn, P., Eckrich, B., Schneidrowski, B., et al. β1-adrenoceptor subtype selective antagonism of esmolol and its major metabolite in vitro and in man. Investigations using tricresylphosphate as red blood cell carboxylesterase inhibitor. Arzneimittelforschung 45(5), 536-541 (1995).