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Finerenone (BAY 94-8862) is a third generation selective, oral active, non-steroidal halocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone showed good selectivity (>500-fold) compared to glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (AR). Finerenone has potential applications in the study of heart and kidney diseases, such as type 2 diabetes and chronic kidney disease.
| Cell Experiment | |
|---|---|
| Cell lines | Human coronary artery smooth muscle cells |
| Preparation method | Cells are incubated with aldosterone with or without finerenone for 24 hours after 24 hours of serum-starvation for the assessment of cell proliferation and apoptosis. Immediately prior to the addition of aldosterone, cells are preincubated with finerenone or vehicle for 30 minutes. |
| Concentrations | 1 nM, 10 nM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | Twelve-week-old MWF, aged-matched normoalbuminuric Wistar rats |
| Formulation | in 10% EtOH, 40% PEG400, 50% water |
| Dosages | 10 mg/kg/day |
| Administration | p.o. |
| Molecular Weight | 378.43 |
| Formula | C21H22N4O3 |
| CAS Number | 1050477-31-0 |
| Solubility (25°C) | DMSO ≥ 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Mineralocorticoid Receptor Products |
|---|
| Spironolactone
Spironolactone (SC9420) is an oral active aldosterone mineralocorticoid receptor antagonist with an IC50 value of 24 nM. Spironolactone is also an androgen receptor antagonist with an IC50 of 77 nM. Spironolactone promotes podocyte autophagy. |
| Potassium canrenoate
Canrenoate potassium is a predrug for the release of Canrenone and an effective antagonist of competitive salt ocorticoid receptor. As a diuretic, Canrenoate potassium is used in the study of hypertension. |
| Osilodrostat
Osilodrostat (LCI699) is a potent, orally active11β-hydroxylase (CYP11B1) inhibitor with an IC50 value of 35 nM. Osilodrostat is a potent, orally aldosterone synthase (CYP11B2) inhibitor with IC50 values of 0.7 nM and 160 nM for human aldosterone synthase and rat aldosterone synthase, respectively. |
| Canrenone
Canrenone is a mineralocorticoid receptor antagonist. |
| Esaxerenone (CS-3150)
Esaxerenone (CS-3150) is a highly potent and selective non-steroidal mineralocorticoid receptor antagonist. |
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