Home Endocrinology & Hormones Mineralocorticoid Receptor inhibitor Esaxerenone (CS-3150) For research use only.

Esaxerenone (CS-3150)

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.

Esaxerenone (CS-3150) Chemical Structure

Esaxerenone (CS-3150) Chemical Structure

CAS No. 1632006-28-0

Purity & Quality Control

Batch: E070401 DMSO]93 mg/mL]false]]]false]]]false Purity: 99.95%
99.95

Esaxerenone (CS-3150) Related Products

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
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]
Cell Research 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.
In Vivo
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]
Animal Research Animal Models bilateral adrenalectomized rat
Dosages 0.3, 1 and 3 mg/kg
Administration o.g.

Chemical Information & Solubility

Molecular Weight 466.48 Formula

C22H21F3N2O4S
CAS No. 1632006-28-0 SDF --
Smiles CC1=C([N](CCO)C=C1C(=O)NC2=CC=C(C=C2)[S](C)(=O)=O)C3=CC=CC=C3C(F)(F)F
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 93 mg/mL ( (199.36 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)


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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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