Nebivolol (hydrochloride)

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Cat No: 23660

Biochemicals - Receptor Pharmacology

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 ove...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

(?R,?'R,2R,2'S)-rel-?,?'-[iminobis(methylene)]bis[6-fluoro-3,4-dihydro-2H-1-benzopyran-2-methanol, monohydrochloride

Correlated keywords:

118457-14-0 R067555 Nebicard Nebilet Nodon ?1AR ?2AR 5HT 5HT1A 5HT2 TGF?1 R-067555 NO platelet-derived transforming fibroblast PDGF-BB

Product Overview:
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.

Size	5 mg
Shipping	dry ice
CAS Number	152520-56-4
Molecular Formula	C₂₂H₂₅F₂NO₄ • HCl
SMILES	FC1=CC=C2C(CC[C@]([C@@H](O)CNC[C@H](O)[C@@]3([H])CCC(C=C(F)C=C4)=C4O3)([H])O2)=C1.Cl
Molecular Weight	441,9
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2903.99
UNSPSC code	12352100

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

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ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.