| Bioactivity | (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]. |
| Target | IC50: 0.8 nM (β1-adrenergic receptor) |
| In Vivo | 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[3]. |
| Name | (Rac)-Nebivolol |
| CAS | 99200-09-6 |
| Formula | C22H25F2NO4 |
| Molar Mass | 405.44 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. 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. [2]. 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. [3]. 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. |