A β1-AR antagonist; binds to β1-ARs (Kd = 100 nM in isolated cardiac myocytes); 34-fold selective for β1- over β2-ARs; inhibits ICa.L and the INa in rat cardiac myocytes (IC50s = 50 and 169 μM

Esmolol (hydrochloride) – 10 mg

Brand:
Cayman
CAS:
81161-17-3
Storage:
-20
UN-No:
Non-Hazardous - /

Esmolol is a β1-adrenergic receptor (β1-AR) antagonist.{36081} It binds to β1-ARs (Kd = 100 nM in isolated cardiac myocytes) and is 34-fold selective for β1- over β2-ARs.{36081,54302} 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.{36081} 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.  

 

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Description

A β1-AR antagonist; binds to β1-ARs (Kd = 100 nM in isolated cardiac myocytes); 34-fold selective for β1- over β2-ARs; inhibits ICa.L and the INa in rat cardiac myocytes (IC50s = 50 and 169 μM, respectively)

Formal name: 4-[2-hydroxy-3-[(1-methylethyl)amino]propoxy]-benzenepropanoic acid, methyl ester, monohydrochloride

Synonyms:  ASL 8052

Molecular weight: 331.8

CAS: 81161-17-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Cardiovascular System|Cardiovascular Diseases|Myocardial Infarction||Research Area|Cardiovascular System|Heart|Arrhythmia||Research Area|Cardiovascular System|Heart|Myocardial Contractility

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