| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
(Rac)-Finerenone targets the mineralocorticoid receptor (MR) through its active enantiomer, Finerenone. Finerenone is a third-generation, selective, nonsteroidal mineralocorticoid receptor antagonist with an IC₅₀ of 18 nM. It displays good selectivity (>500-fold) for the androgen receptor (AR) and the progesterone receptor. By blocking the mineralocorticoid receptor, Finerenone inhibits aldosterone-mediated effects on sodium reabsorption, inflammation, and fibrosis. Its nonsteroidal nature and high selectivity may offer advantages over steroidal MR antagonists in terms of side effect profiles.
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| ln Vitro |
In vitro, Finerenone demonstrates potent mineralocorticoid receptor antagonist activity with an IC₅₀ of 18 nM. It displays good selectivity (>500-fold) for the androgen receptor and progesterone receptor, indicating a favorable selectivity profile. The compound's activity is assessed in cell-based reporter assays using mineralocorticoid response element (MRE)-luciferase constructs. Its antagonist activity is evaluated by its ability to inhibit aldosterone-induced transcriptional activation. The racemic mixture is used as a reference standard for analytical purposes.
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| ln Vivo |
In vivo, Finerenone is an orally bioavailable, nonsteroidal mineralocorticoid receptor antagonist. It has been investigated for the treatment of cardiovascular and renal diseases, including chronic kidney disease and heart failure. The compound's nonsteroidal nature and high selectivity may offer advantages over steroidal MR antagonists in terms of side effect profiles. It has undergone clinical development for various indications. The racemic mixture (Rac)-Finerenone is used as an analytical reference standard.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for (Rac)-Finerenone typically involve competitive binding experiments using mineralocorticoid receptor and radiolabeled or fluorescently labeled aldosterone as tracer. Finerenone's binding affinity to the mineralocorticoid receptor is assessed, with an IC₅₀ of 18 nM determined through dose-response binding experiments. Selectivity is assessed by parallel binding assays using androgen receptor and progesterone receptor. Assays are conducted in buffered solutions at physiological pH with appropriate receptor preparations. Binding affinity is expressed as IC₅₀ or Kd values.
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| Cell Assay |
In vitro cell-based assays for (Rac)-Finerenone utilize cell lines expressing mineralocorticoid receptor to assess its antagonist activity. Cells are treated with varying concentrations of the compound for 24-48 hours in the presence of aldosterone. MR-mediated transcriptional activity is evaluated using reporter gene assays with MRE-luciferase constructs. The compound's antagonist activity is assessed by its ability to inhibit aldosterone-induced transcriptional activation. Selectivity is confirmed using parallel assays with androgen and progesterone receptors. Standard cell culture conditions (37°C, 5% CO₂) with appropriate media are employed.
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| Animal Protocol |
In vivo animal studies with Finerenone typically involve administration of the compound to rodent models of cardiovascular or renal diseases. Potential study designs include models of chronic kidney disease, heart failure, or hypertension. Typical endpoints would include measurements of blood pressure, renal function, markers of inflammation and fibrosis, and pharmacokinetic profiling. The compound's efficacy and safety have been evaluated in preclinical studies supporting its clinical development. All procedures must comply with institutional animal care and use guidelines.
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| ADME/Pharmacokinetics |
Finerenone is orally bioavailable with favorable pharmacokinetic properties. It has a molecular weight of 378.42 g/mol and a molecular formula of C₂₁H₂₂N₄O₃. Its chemical name is 4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide. As a nonsteroidal MR antagonist, it may have favorable pharmacokinetic properties compared to steroidal antagonists. The racemic mixture is used as an analytical reference standard.
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| Toxicity/Toxicokinetics |
Finerenone has been evaluated in clinical trials for cardiovascular and renal indications. As an investigational drug, it has undergone comprehensive toxicological evaluation in preclinical studies. Common adverse effects may include hyperkalemia, hypotension, and electrolyte imbalances. The compound should be used with caution in patients with renal impairment or those taking other medications that affect potassium levels. Patients should be monitored for electrolyte imbalances and renal function.
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| References | |
| Additional Infomation |
(Rac)-Finerenone ((Rac)-BAY 94-8862) (CAS#: 1050477-27-4) has a molecular formula of C₂₁H₂₂N₄O₃ and a molecular weight of 378.42 g/mol. Its chemical name is 4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide. It is the racemate of Finerenone. Finerenone is a third-generation, selective, orally bioavailable, nonsteroidal MR antagonist (IC₅₀ = 18 nM). It displays good selectivity (>500-fold) for AR and progesterone receptor. (Rac)-Finerenone is used as an analytical reference standard.
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| Molecular Formula |
C21H22N4O3
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|---|---|
| Molecular Weight |
378.42
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| Exact Mass |
378.169
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| CAS # |
1050477-27-4
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| Related CAS # |
Finerenone;1050477-31-0
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| PubChem CID |
24993045
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| Appearance |
White to off-white solid powder
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| LogP |
3.823
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
28
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| Complexity |
670
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCOC1=NC=C(C2=C1C(C(=C(N2)C)C(=O)N)C3=C(C=C(C=C3)C#N)OC)C
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| InChi Key |
BTBHLEZXCOBLCY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H22N4O3/c1-5-28-21-18-17(14-7-6-13(9-22)8-15(14)27-4)16(20(23)26)12(3)25-19(18)11(2)10-24-21/h6-8,10,17,25H,5H2,1-4H3,(H2,23,26)
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| Chemical Name |
4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide
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| Synonyms |
(Rac)-BAY-94-8862; (Rac)-BAY94-8862; (Rac)-BAY 94-8862
1050477-27-4; 4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide; DTXSID201035670; RefChem:514119; DTXCID30912349;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 62.5 mg/mL (165.2 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.50 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.50 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.50 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6426 mL | 13.2128 mL | 26.4257 mL | |
| 5 mM | 0.5285 mL | 2.6426 mL | 5.2851 mL | |
| 10 mM | 0.2643 mL | 1.3213 mL | 2.6426 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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