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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Mineralocorticoid Receptor Products |
|---|
| Lorundrostat
Lorundrostat is an aldosterone synthase inhibitor and is used in studies related to hypertension. |
| LY2623091
LY2623091 is a salicorticoid receptor (MR) antagonist that may be used in studies related to chronic kidney disease and hypertension. |
| Desoxycorticosterone pivalate
Desoxycorticosterone pivalate (DOCP) is a salt corticosteroid that may be used in studies related to primary hypoadrenocorticism (PH). |
| Ocedurenone
Ocedurenone is a novel nonsteroidal salicorticoid receptor (MR) antagonist that may be used in studies related to kidney disease. |
| Baxdrostat
Baxdrostat is a aldosterone synthase inhibitor. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
