Products Description
English name：Finerenone
CAS number：1050477-31-0
Molecular formula: C21H22N4O3
Molecular weight: 378.42
EINECS number:
Related category
Chemical raw materials; Active molecule; Pharmaceutical raw materials; Chemical reagent; Reagent; Raw materials; Superior products; Biological reagent; Finelidone intermediate; Pharmaceutical raw material
Mol file：1050477-31-0.mol
Structural formula:
Properties of finelidone
Boiling point: 554.7±50.0°C(Predicted)
Density: 1.29±0.1g/cm3(Predicted)
Storage condition: -20°C
Solubility: DMF: 10 mg/mlDMSO: 3 chemicalbookmg/ml of ethanol: insolPBS (pH7.2) : insol
Form: solid
Acidity coefficient (pKa) : 14.76±0.40(Predicted)
Color: White to beige
Maximum wavelength (λmax) : 255nm
InChI：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)/t17-/m1/s1
InChIKey：BTBHLEZXCOBLCY-QGZVFWFLSA-N
SMILES：N1C2=C(C(OCC)=NC=C2C)[C@H](C2=CC=C(C#N)C=C2OC)C(C(N)=O)=C1C
Use and synthesis of finelidone
Intro
Finelidone is a novel salocorticoid receptor antagonist, which has the effect of delaying the progression of chronic kidney disease. Some of you may know of two other salt corticosteroid receptor antagonists: spironolactone, a diuretic blood pressure medication, and Eplenone. Finelidone is their sibling, the third generation of salocorticoid receptor antagonists just developed after the two.
Action mechanism
The salt corticosteroid receptor is one of the reasons for the increase of urinary protein and the deterioration of renal function.
Salocorticoid receptors can be over-activated by factors such as increased aldosterone, causing sodium retention, increasing blood pressure, promoting kidney inflammation, and accelerating kidney fibrosis (kidney failure). The antagonism of Chemicalbook salt corticosteroid receptor to improve inflammation and fibrosis has been a key therapeutic target in the field of nephrology in recent years, and finalizone was the first real breakthrough.
Use
Finelidone is the first non-steroidal selective salt corticosteroid receptor antagonist, which can be used in the treatment of diabetic nephropathy, chronic nephropathy and end-stage nephropathy. It can reduce proteinuria and improve glomerular filtration rate.
Biological activity
Finerenone (FIN, BAY94-8862) is a highly selective, the activity of oral mineralocorticoidreChemicalbookceptor non-steroidal antagonists (MR), IC50 alue concentration of 18 nm. Finerenone has the potential to study cardio-renal diseases such as type 2 diabetes and chronic kidney disease.
Target point
Target Value
MR
18 nM
TargetValue MR (Cell-free assay)
In vivo study
Finerenone (BAY 94-8862) lowers albuminuria by >40% and significantly reduces systolic blood pressure (SBP) in Munich Wistar Frömter (MWF) rat.
Animal Model: Twelve-week-old MWF rat
Dosage: 10 mg/kg
Administration: P.o.; daily for 4 weeks
Result: Significantly reduced SBP in MWF rats; led to a significant reduction (>40%) in albuminuria in the MWF model. Animal Model: Twelve-week-old MWF rat
Dosage: 10 mg/kg
Administration: P.o.; daily for 4 weeks
Result: Significantly reduced SBP in MWF rats; led to a significant reduction (>40%) in albuminuria in the MWF model.
Side effect
Hyperkalemia, hypotension and hyponatremia, pruritus, and decreased glomerular filtration rate occur in more than 1% of patients.
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