Esaxerenone (CS-3150)

Catalog No.E0704 Batch:E070401

Technical Data

Formula	C₂₂H₂₁F₃N₂O₄S
Molecular Weight	466.48	CAS No.	1632006-28-0
Solubility (25°C)*	In vitro	DMSO	93 mg/mL (199.36 mM)


* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

Esaxerenone (CS-3150), a selective nonsteroidal mineralocorticoid receptor (MR) antagonist, binds to mineralocorticoid receptor and inhibits (3)H-aldosterone binding to mineralocorticoid receptor with an IC50 value of 9.4 nM. Esaxerenone (CS-3150) also has the property of increasing the likelihood of albuminuria returning to normal levels and reducing progression of albuminuria to higher levels.

Targets

Mineralocorticoid Receptor ^[1]
(in the radioligand-binding assay)

9.4 nM

In vitro

Esaxerenone is a selective nonsteroidal mineralocorticoid receptor antagonist, which inhibits aldosterone-induced transcriptional activation of human mineralocorticoid receptor with no agonistic effect on mineralocorticoid receptor, and has no antagonistic or agonistic effect on glucocorticoid receptor, androgen receptor and progesterone receptor even at the high concentration of 5 μM.^[1]

In vivo

In adrenalectomized rats, single oral administration of esaxerenone suppressed aldosterone-induced decrease in urinary Na(+)/K(+) ratio, an index of in vivo mineralocorticoid receptor activation, and this suppressive effect is more potent and longer-lasting than that of spironolactone and eplerenone.^[1]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines 293 A cells Concentrations 1 nM Incubation Time 24 h Method For the transient transfection experiments, 293 A cells are inoculated on 100 mm dishes (4.5×10⁶ cells/dish) and cultured for 24 h in DMEM with 10% heat-inactivated FBS in 5% CO2 at 37 ℃. Then, the cells are co-transfected with each of expression plasmid and 3×GRE-Luc2P by lipofection using Lipofectamine 2000. After transfection, the cells are harvested and transferred into 96-well plates (1.0×10⁴ cells/well) containing a DMEM with 10% heat-inactivated charcoal-stripped FBS followed by incubation for 24 h. Serial dilutions of esaxerenone with or without 1 nM of the corresponding ligands for each receptor are added and further incubated for approximately 24 h. The luciferase activity of each well is measured in a multimode assay system.
Animal Study:^{^[1]}	Animal Models bilateral adrenalectomized rat Dosages 0.3, 1 and 3 mg/kg Administration o.g.

Cell Assay:^{^[1]}

Cell lines
293 A cells
Concentrations
1 nM
Incubation Time
24 h
Method
For the transient transfection experiments, 293 A cells are inoculated on 100 mm dishes (4.5×10⁶ cells/dish) and cultured for 24 h in DMEM with 10% heat-inactivated FBS in 5% CO2 at 37 ℃. Then, the cells are co-transfected with each of expression plasmid and 3×GRE-Luc2P by lipofection using Lipofectamine 2000. After transfection, the cells are harvested and transferred into 96-well plates (1.0×10⁴ cells/well) containing a DMEM with 10% heat-inactivated charcoal-stripped FBS followed by incubation for 24 h. Serial dilutions of esaxerenone with or without 1 nM of the corresponding ligands for each receptor are added and further incubated for approximately 24 h. The luciferase activity of each well is measured in a multimode assay system.

Animal Study:^{^[1]}

Animal Models
bilateral adrenalectomized rat
Dosages
0.3, 1 and 3 mg/kg
Administration
o.g.

References

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SHIPPING AND STORAGE
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