Home Endocrinology & Hormones Mineralocorticoid Receptor inhibitor Esaxerenone (CS-3150)

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Esaxerenone (CS-3150) Mineralocorticoid Receptor inhibitor

Cat.No.E0704

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. This compound 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) Mineralocorticoid Receptor inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 466.48

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 93 mg/mL (199.36 mM)
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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 466.48 Formula

C22H21F3N2O4S

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1632006-28-0 -- Storage of Stock Solutions

Mechanism of Action

Targets/IC50/Ki
Mineralocorticoid Receptor
(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.
In vivo

In adrenalectomized rats, single oral administration of esaxerenone (CS-3150) 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.
References

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