A potent and selective β1-AR antagonist (IC50s = 7.41 and 251 nM for β1- and β2-ARs

Nebivolol (hydrochloride) – 5 mg

Brand:
Cayman
CAS:
152520-56-4
Storage:
-20
UN-No:
Non-Hazardous - /

Nebivolol is a potent and selective β1-adrenergic receptor (β1-AR) antagonist (IC50s = 7.41 and 251 nM for β1- and β2-ARs, respectively in a radioligand binding assay using rabbit lung membrane preparations).{38519} It is also selective for β1-ARs over serotonin 5-HT1A and 5-HT2, α1- and α2-adrenergic, histamine H1, and dopamine D2 receptors (IC50s = 27.5 and 2,239, 3,162 and >10,000, 5,623, and 10,000 nM, respectively). Nebivolol inhibits cAMP accumulation induced by norepinephrine (Item No. 16673) in primary rat cardiac cells (IC50 = 22 nM) and induces vasodilation in mouse renal arteries via a nitric oxide- and cGMP-dependent mechanism (EC50 = 11.36 μM).{38520,38521} It decreases contraction of isolated human left ventricular trabeculae induced by isoproterenol (Item No. 15592; IC50 = 7.0 μM) but does not exert intrinsic sympathomimetic activity (ISA).{38522} Nebivolol inhibits proliferation of human coronary artery smooth muscle cells (HCASMCs) in the presence and absence of growth factors (IC50s = 6.1, 6.8, 6.4, and 7.7 μM for HCASMCs grown in media containing no growth factor, PDGFBB, basic FGF, and TGF-β1, respectively).{38523} Formulations containing nebivolol have been used to treat hypertension.  

 

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Description

A potent and selective β1-AR antagonist (IC50s = 7.41 and 251 nM for β1- and β2-ARs, respectively in a radioligand binding assay using rabbit lung membrane preparations); selective for β1-ARs over 5-HT1A and 5-HT2, α1- and α2-adrenergic, H1, and D2 receptors (IC50s = 27.5 and 2,239, 3,162 and >10,000, 5,623, and 10,000 nM, respectively); inhibits cAMP accumulation induced by norepinephrine in primary rat cardiac cells (IC50 = 22 nM); induces vasodilation in mouse renal arteries via a nitric oxide- and cGMP-dependent mechanism (EC50 = 11.36 μM); decreases contraction of isolated human left ventricular trabeculae induced by isoproterenol (IC50 = 7.0 μM) but does not exert ISA; inhibits proliferation of HCASMCs in the presence and absence of growth factors (IC50s = 6.1, 6.8, 6.4, and 7.7 μM for HCASMCs grown in media containing no growth factor, PDGFBB, basic FGF, and TGF-β1, respectively),

Formal name: (αR,α’R,2R,2’S)-rel-α,α’-[iminobis(methylene)]bis[6-fluoro-3,4-dihydro-2H-1-benzopyran-2-methanol, monohydrochloride

Synonyms: 

Molecular weight: 441.9

CAS: 152520-56-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Cardiovascular System|Heart|Arrhythmia||Research Area|Cardiovascular System|Heart|Myocardial Contractility||Research Area|Cardiovascular System|Kidney & Renal Disease||Research Area|Cardiovascular System|Vasculature|Angiogenesis||Research Area|Cardiovascular System|Vasculature|Vasodilation

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