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Chemical Structure| 1632006-28-0 Chemical Structure| 1632006-28-0

Structure of Esaxerenone
CAS No.: 1632006-28-0

Chemical Structure| 1632006-28-0

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Esaxerenone is an aldosterone receptor antagonist. Esaxerenone may be potential useful for preventing or treating hypertension or disease caused by hypertension.

Synonyms: CS-3150; XL-550

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Product Details of Esaxerenone

CAS No. :1632006-28-0
Formula : C22H21F3N2O4S
M.W : 466.47
SMILES Code : O=C(C1=CN(CCO)C(C2=CC=CC=C2C(F)(F)F)=C1C)NC3=CC=C(S(=O)(C)=O)C=C3
Synonyms :
CS-3150; XL-550
MDL No. :N/A

Safety of Esaxerenone

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Isoform Comparison

Biological Activity

In Vitro:

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

In Vivo:

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

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02448628 Hypertension PHASE2 COMPLETED 2025-12-15 Osaka, 530-0001, Japan
NCT02885662 Primary Aldosteronism COMPLETED 2017-07-20 Japan Organaization of Occupat... More >>ional Health and Safety(JOHAS), Yokohama Rosai Hospital, Yokohama, Kanagawa, 222-0036, Japan Less <<
NCT02722265 Essential Hypertension PHASE3 COMPLETED 2017-07-08 Osaka, Japan
NCT02807987 Hypertension With Moderate Ren... More >>al Impairment Less << PHASE3 COMPLETED 2017-05-15 Nagano, Japan
NCT02808026 Severe Hypertension PHASE3 COMPLETED 2025-02-17 Sapporo, Japan
NCT02807974 Hypertension PHASE3 COMPLETED 2025-03-17 Sanuki-shi, Kagawa, Japan

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.14mL

0.43mL

0.21mL

10.72mL

2.14mL

1.07mL

21.44mL

4.29mL

2.14mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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