Finerenone

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Finerenone (BAY 94-8862) 是一种有效的、选择性的、口服的盐皮质激素受体 (MR) 拮抗剂，IC50 为 18 nM。

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.

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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 ratDosage: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 ratDosage: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.

BAY 94-8862 | BAY 948862

Nuclear Receptor/Transcription Factor

MLR

MLR

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1050477-31-0

378.432

C21H22N4O3

>98% (HPLC)

In Vitro:?DMSO : 200 mg/mL (528.51 mM)

O=C(C1=C(C)NC2=C(C(OCC)=NC=C2C)[C@@H]1C3=CC=C(C#N)C=C3OC)N

(4S)-4-(4-Cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide

(-20℃)

With Ice Pack

≥ 2 years