Esaxerenone is recognized as a highly effective and selective antagonist for the non-steroidal mineralocorticoid receptor[1].
Esaxerenone 细胞实验
Cell Line
Concentration
Treated Time
Description
References
HEK293T cells
5 μmol/L
24 hours
To investigate the effect of Esaxerenone on the transcriptional activity of the MR-p65-STAT3 complex. Results showed that Esaxerenone significantly attenuated the p65-driven IL-6 promoter activity enhanced by co-expression of MR and STAT3.
J Am Heart Assoc. 2024 Sep 17;13(18):e030941
RAW264.7 cells
1 μmol/L
1 hour
To evaluate the inhibitory effect of Esaxerenone on lipopolysaccharide-induced inflammatory response. Results showed that Esaxerenone significantly attenuated lipopolysaccharide-induced IL-6 and TNF-α mRNA expression.
J Am Heart Assoc. 2024 Sep 17;13(18):e030941
Esaxerenone 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Dahl salt-sensitive hypertensive rats
High-salt diet-induced hypertension and cardiac hypertrophy model
Dietary administration
0.001% (w/w)
Daily administration for 4 weeks
To evaluate the cardioprotective effects of Esaxerenone. Results showed that Esaxerenone significantly improved cardiac function, reduced cardiac fibrosis, inflammation, and oxidative stress.
Int J Mol Sci. 2021 Feb 19;22(4):2069
C57BL/6 mice
Aldosterone-infused model
Diet administration
1 mg/kg diet
Continued for 12 weeks
To investigate the effect of Esaxerenone on aldosterone-induced renal injury, angiogenesis, and endothelial-mesenchymal transition, results showed Esaxerenone inhibited renal angiogenesis and endothelial-mesenchymal transition.
Int J Mol Sci. 2023 Jul 21;24(14):11766
Female Sprague-Dawley rats
Intracranial aneurysm model
Oral
1 mg/kg/day
Once daily for 6 weeks
ESA significantly prolonged SAH-free survival and improved abnormal morphological changes in the vascular wall, reducing the expression levels of RAGE, MR, and NFκB.
J Neuroinflammation. 2022 Jun 20;19(1):161
Wistar rats
Aldosterone-induced inflammatory vascular lesion model
Dietary addition
1 mg/kg/day
Once daily for 12 weeks
To verify the protective effect of Esaxerenone on aldosterone-induced vascular inflammatory injury
Int J Mol Sci. 2025 Apr 3;26(7):3345
Sprague Dawley rats
Ischemia–reperfusion injury (IRI) model
Oral
3 mg/kg/day
Once daily for 6 weeks
Esaxerenone suppressed the rise in blood pressure and increased urinary albumin excretion in IRI/NaCl and IRI/Aldo rats and ameliorated renal tissue damage.
Int J Mol Sci. 2022 Jul 15;23(14):7831
C57BL/6J mice
Myocardial infarction model
Oral
0.003% w/w
Once daily for 15 days
To evaluate the effect of Esaxerenone on cardiac function and inflammatory response after myocardial infarction. Results showed that Esaxerenone significantly improved cardiac function, attenuated cardiac fibrosis, and reduced inflammatory response.
J Am Heart Assoc. 2024 Sep 17;13(18):e030941
Dahl salt-sensitive hypertensive rats
High-salt diet-induced hypertension model
Oral
0.001% (w/w)
Daily administration for 4 weeks
Evaluate the effects of Esaxerenone on BP and sodium balance, results showed Esaxerenone significantly reduced BP and improved sodium excretion
Int J Mol Sci. 2022 Aug 10;23(16):8915
Esaxerenone 动物研究
Animal study
Following a single oral dose of Esaxerenone at 0.1, 0.3, 1, and 3 mg/kg, there is a dose-dependent increase in both the maximum plasma concentration (Cmax) and the area under the plasma concentration-time curve (AUC). The Tmax, or the time to reach Cmax, varies from 2.0 to 4.5 hours. With intravenous doses of Esaxerenone at the same concentrations, the total body clearance (CL) ranges from 3.53 to 6.69 mL/min/kg and the steady-state distribution volume (Vss) from 1.47 to 2.49 L/kg in rats, while in cynomolgus monkeys, the CL is 2.79 to 3.69 mL/min/kg and the Vss is 1.34 to 1.54 L/kg. Post-administration, up to 168 hours, rats excrete 3.9% of the radioactivity in urine and 91.4% in feces, totaling 95.2%. In monkeys, 11.5% is excreted in urine, 82.3% in feces, and 93.9% in total within the same timeframe[1].
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