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

research use only

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

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability

Quality Control

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

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

Solubility

In vitro
Batch:

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

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
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 (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.[1]
References

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.