(Rac)-Nebivolol-d₂,¹⁵N  (Synonyms: (Rac)-R 065824-d₂,¹⁵N)

(Rac)-Nebivolol-d₂,¹⁵N is ¹⁵N and deuterated labeled (Rac)-Nebivolol (HY-B0203B). (Rac)-Nebivolol ((Rac)-R 065824) is a racemic isomer of Nebivolol. Nebivolol is a selective β1-adrenergic receptor antagonist with an IC₅₀ value of 0.8 nM. Nebivolol can prevent up-regulation of Nox2/NADPH oxidase and lipoperoxidation in the early stages of ethanol-induced cardiac toxicity. Vasodilatory activity^[1][2].

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Nebivolol (10 mg/kg; daily for 7 days) markedly improves endothelial dysfunction and increases P-VASP levels; prevents NOS III uncoupling; significantly inhibit NADPH oxidase in Angiotensin II-treated rats^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

408.44

C₂₂H₂₃D₂F₂¹⁵NO₄

99200-09-6

FC1=CC=C2OC(C(C[15NH]CC(C3OC4=CC=C(C=C4C([2H])C3)F)O)O)CC([2H])C2=C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.  [Content Brief]

  [2]. do Vale GT, et al. Nebivolol Prevents Up-Regulation of Nox2/NADPH Oxidase and Lipoperoxidation in the Early Stages of Ethanol-Induced Cardiac Toxicity. Cardiovasc Toxicol. 2021 Mar;21(3):224-235.  [Content Brief]

  [3]. Cockcroft JR, et al. Nebivolol vasodilates human forearm vasculature: evidence for an L-arginine/NO-dependent mechanism. J Pharmacol Exp Ther. 1995 Sep;274(3):1067-71.  [Content Brief]

  [4]. Oelze M, et al. Nebivolol inhibits superoxide formation by NADPH oxidase and endothelial dysfunction in angiotensin II-treated rats. Hypertension. 2006 Oct;48(4):677-84.  [Content Brief]