(±)-Nebivolol-<wbr/>d<sub>4</sub> (hydro<wbr/>chloride)

(±)-Nebivolol-d4 (hydrochloride)

CAT N°: 26659
Price:

270.00 229.50

(±)-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 ?1-adrenergic receptor (?1-AR; IC50 = 7.41 nM).{38519} It is selective for ?1- over ?2-ARs (IC50 = 251 nM), as well as the serotonin (5-HT) receptor subtypes 5-HT1A and 5-HT2 and the ?1- and ?2-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-?1, 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.

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