Finerenone

SKU: orb1941115

Description

Finerenone (BAY 94-8862) is a potent, selective, orally available mineralocorticoid receptor (MR) antagonist with IC50 of 18 nM; displays excellent selectivity (>500-fold) versus GR, AR, and PR, also shows no L type Ca2+ channel activity; elicits a significant and dose-dependent increase in the urinary sodium/potassium ratio in vivo, with a MED of 0.3 mg kg1 p.o.; exhibits three- to tenfold greater potency and higher efficacy in acute rat natriuresis model compared with eplerenone, demonstrates potential for the treatment of chronic heart failure (CHF).Heart FailurePhase 3 Clinical(In Vivo):Finerenone (BAY 94-8862) lowers albuminuria by >40% and significantly reduces systolic blood pressure (SBP) in Munich Wistar Fr mter (MWF) rat.

Key Properties

• CAS Number: 1050477-31-0
• MW: 378.432
• Purity: >98% (HPLC)
• Formula: C₂₁H₂₂N₄O₃
• SMILES: O=C(C1=C(C)NC2=C(C(OCC)=NC=C2C)[C@@H]1C3=CC=C(C#N)C=C3OC)N
• Target: MLR
• Solubility: In Vitro: DMSO : 200 mg/mL (528.51 mM)

Bioactivity

• In Vivo:
  Finerenone (BAY 94-8862) lowers albuminuria by >40% and significantly reduces systolic blood pressure (SBP) in Munich Wistar Fr mter (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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BAY 94-8862 | BAY 948862

Quick Database Links

Gene Symbol

MLR