Finerenone (Synonyms: BAY 94-8862) |
Catalog No.GC60842
One-Click Copy Product Info
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Finerenone (BAY 94-8862) is a third-generation selective, orally active, nonsteroidal mineralocorticoid receptor (MR) antagonist with an IC50 of 18 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1050477-31-0
Sample solution is provided at 25 µL, 10mM.
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Finerenone (BAY 94-8862) is a third-generation selective, orally active, nonsteroidal mineralocorticoid receptor (MR) antagonist with an IC50 of 18 nM[1]. Finerenone is more selective for MR than for glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (AR) (>500-fold)[2]. Finerenone is mainly used in the study of cardiorenal diseases, such as type 2 diabetes and chronic kidney disease[3].
In vitro, treatment of neonatal rat cardiomyocytes (NRCM) with finerenone (20 nM) reduced apoptosis stimulated by high glucose and high fatty acids, improved cardiomyocyte metabolism and reduced ROS generation via the PPARγ/CD36 pathway[4].
In vivo, oral treatment of chronic kidney disease model (MWF) and wild-type rats with finerenone (10mg/kg) significantly reduced albuminuria in MWF rats, increased endothelial nitric oxide utilization, and significantly improved endothelial function in MWF rats[5]. Finerenone (5mg/kg) was intraperitoneally injected into mice with induced retinopathy (OIR), which reduced retinal systolic pressure, gliosis, vascular leakage, and microglia/macrophage density[6]. Finerenone (10 mg/kg) was orally administered into mice with cardiac/renal inflammation model, which significantly improved the upregulation of infiltrating renal RORγt γδ-positive T cells induced by deoxycorticosterone acetate (DOCA) salt exposure and prevented cardiac and renal damage[7].
References:
[1] Liu L C Y, Schutte E, Gansevoort R T, et al. Finerenone: third-generation mineralocorticoid receptor antagonist for the treatment of heart failure and diabetic kidney disease[J]. Expert opinion on investigational drugs, 2015, 24(8): 1123-1135.
[2] Bădilă E. The expanding class of mineralocorticoid receptor modulators: New ligands for kidney, cardiac, vascular, systemic and behavioral selective actions[J]. Acta Endocrinologica (Bucharest), 2020, 16(4): 487.
[3] Agarwal R, Filippatos G, Pitt B, et al. Cardiovascular and kidney outcomes with finerenone in patients with type 2 diabetes and chronic kidney disease: the FIDELITY pooled analysis[J]. European heart journal, 2022, 43(6): 474-484.
[4] Jin T, Fu X, Liu M, et al. Finerenone attenuates myocardial apoptosis, metabolic disturbance and myocardial fibrosis in type 2 diabetes mellitus[J]. Diabetology & Metabolic Syndrome, 2023, 15(1): 87.
[5] González-Blázquez R, Somoza B, Gil-Ortega M, et al. Finerenone attenuates endothelial dysfunction and albuminuria in a chronic kidney disease model by a reduction in oxidative stress[J]. Frontiers in Pharmacology, 2018, 9: 1131.
[6] Jerome J R, Deliyanti D, Suphapimol V, et al. Finerenone, a non-steroidal mineralocorticoid receptor antagonist, reduces vascular injury and increases regulatory T-cells: Studies in rodents with diabetic and neovascular retinopathy[J]. International Journal of Molecular Sciences, 2023, 24(3): 2334.
[7] Luettges K, Bode M, Diemer J N, et al. Finerenone reduces renal RORγt γδ T cells and protects against cardiorenal damage[J]. American Journal of Nephrology, 2022, 53(7): 552-564.
| Cell experiment [1]: | |
Cell lines | Neonatal rat cardiomyocytes |
Preparation Method | Neonatal rat cardiomyocytes (NRCMs) were extracted for cell culture, and the medium used was DMEM) medium. Hyperlipidemia or hyperglycemia regulation was mimicked by incubation with high concentrations of common saturated FFA (sodium palmitate, 16:0, 0.3 mM) or glucose (D-glucose, 33 mM). Palmitate was previously conjugated with BSA in a 3:1 molar ratio. In control cells, BSA was added as described but in the absence of palmitate. Finerenone (20nM) was added 1 h before stimulation. |
Reaction Conditions | 20nM; 1 h |
Applications | Finerenone reduces the apoptosis of cardiomyocytes stimulated by high glucose and high fatty acid. Finerenone improves cardiomyocyte metabolism and reduces ROS generation through PPARγ/CD36 pathway. |
| Animal experiment [2]: | |
Animal models | Male Wistar and MWF rats |
Preparation Method | Twelve-week-old male Wistar and MWF rats were housed in groups of two under controlled dark-light cycles, temperature conditions and with food and water available ad libitum. Animals were randomly grouped to receive finerenone (10mg/kg/day in 10% EtOH, 40% PEG400, 50% water; W-FIN; MWF-FIN) or vehicle (10% EtOH, 40% PEG400, 50% water; W-C; MWF-C) during 4 weeks by once daily oral gavage. Last oral administration of FIN was performed the day before sacrifice. |
Dosage form | 10mg/kg; p.o. |
Applications | Finerenone lead to a significant reduction (>40%) in albuminuria in the MWF mode, while normoalbuminuria was not affected in Wistar rats. |
References: [1] Jin T, Fu X, Liu M, et al. Finerenone attenuates myocardial apoptosis, metabolic disturbance and myocardial fibrosis in type 2 diabetes mellitus[J]. Diabetology & Metabolic Syndrome, 2023, 15(1): 87. [2] González-Blázquez R, Somoza B, Gil-Ortega M, et al. Finerenone attenuates endothelial dysfunction and albuminuria in a chronic kidney disease model by a reduction in oxidative stress[J]. Frontiers in Pharmacology, 2018, 9: 1131. | |
| Cas No. | 1050477-31-0 | SDF | |
| Synonyms | BAY 94-8862 | ||
| Canonical SMILES | O=C(C1=C(C)NC2=C(C(OCC)=NC=C2C)[C@@H]1C3=CC=C(C#N)C=C3OC)N | ||
| Formula | C21H22N4O3 | M.Wt | 378.42 |
| Solubility | DMSO : 100 mg/mL (DMSO moisture absorption will reduce the solubility of the compound, please use a new DMSO; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6426 mL | 13.2128 mL | 26.4257 mL |
| 5 mM | 528.5 μL | 2.6426 mL | 5.2851 mL |
| 10 mM | 264.3 μL | 1.3213 mL | 2.6426 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)