(R)-Finerenone ((R)-BAY 94-8862) is the R-isomer of Finerenone. Finerenone is a third-generation selective, orally active, non-steroidal mineralocorticoid receptor (MR) antagonist (IC50 = 18 nM). Compared with glucocorticoid receptors (GR), androgen receptors (AR), and progesterone receptors (AR), Finerenone shows good selectivity (> 500-fold). Finerenone has potential application prospects in studies of heart and kidney diseases, such as type 2 diabetes and chronic kidney disease [1] [2].
In Vitro, The R-isomer typically differs in stereoconfiguration from the parent molecule and may exhibit retained or diminished activity, altered toxicity, or differences in pharmacokinetic behavior; in some chiral drugs, the R-form constitutes the primary active or toxic component.
References:
[1]. Bärfacker L, et al. Discovery of BAY 94-8862: a nonsteroidal antagonist of the mineralocorticoid receptor for the treatment of cardiorenal diseases. ChemMedChem. 2012;7(8):1385-1403.
[2]. González-Blázquez R, et al. Finerenone Attenuates Endothelial Dysfunction and Albuminuria in a Chronic Kidney Disease Model by a Reduction in Oxidative Stress. Front Pharmacol. 2018;9:1131. Published 2018 Oct 9.
In Vitro, The R-isomer typically differs in stereoconfiguration from the parent molecule and may exhibit retained or diminished activity, altered toxicity, or differences in pharmacokinetic behavior; in some chiral drugs, the R-form constitutes the primary active or toxic component.
References:
[1]. Bärfacker L, et al. Discovery of BAY 94-8862: a nonsteroidal antagonist of the mineralocorticoid receptor for the treatment of cardiorenal diseases. ChemMedChem. 2012;7(8):1385-1403.
[2]. González-Blázquez R, et al. Finerenone Attenuates Endothelial Dysfunction and Albuminuria in a Chronic Kidney Disease Model by a Reduction in Oxidative Stress. Front Pharmacol. 2018;9:1131. Published 2018 Oct 9.