Product description
(+-)-Nebivolol-d4 is intended for use as an internal standard for the quantification of nebivolol (Item No. 23660) by GC- or LC-MS. Nebivolol is an antagonist of the B1-adrenergic receptor (B1-AR; IC50 = 7.41 nM).{38519} It is selective for B1- over B2-ARs (IC50 = 251 nM), as well as the serotonin (5-HT) receptor subtypes 5-HT1A and 5-HT2 and the a1- and a2-adrenergic, histamine H1, and dopamine D2 receptors (IC50s = 27.5, 2,239, 3,162, >10,000, 5,623, and 10,000 nM, respectively). Nebivolol induces vasodilation in isolated mouse renal arteries (EC50 = 11.36 ?M) and decreases contraction of isolated human left ventricular trabeculae induced by isoproterenol (Item No. 15592; IC50 = 7 ?M).{38521,38522} Nebivolol inhibits proliferation of primary 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 ?M for HCASMCs grown in media containing no growth factor, PDGF-BB, basic FGF, and TGF-B1, respectively).{38523} It is also an inhibitor of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (Mpro), also known as 3C-like protease (3CLpro; IC50 = 60.2 µg/ml), and inhibits SARS-CoV-2 pathogenicity in vitro (IC50 = 0.03 µg/ml).{64706} Formulations containing nebivolol have been used in the treatment of hypertension.
Specifications
CAS number
2701283-32-9
Supplier
Cayman Chemical
Shipping & storage
Shipping condition
Dry Ice
Storage temperature
-20°C

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(+-)-Nebivolol-d4 (hydrochloride)

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