Esaxerenone (Synonyms: CS-3150; XL-550)

Name: Esaxerenone
Brand: MedChemExpress
SKU: HY-100471
Rating: 5.0 (2 reviews)

Cat. No.: HY-100471 Purity: 99.93%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Esaxerenone (CS-3150) is a highly potent and selective non-steroidal mineralocorticoid receptor antagonist.

For research use only. We do not sell to patients.

Esaxerenone Chemical Structure

CAS No. : 1632006-28-0

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 198	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 198	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 80	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 180	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 290	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 560	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 890	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1400	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 2 publication(s) in Google Scholar

2 Publications Citing Use of MCE Esaxerenone

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

Esaxerenone (CS-3150) is a highly potent and selective non-steroidal mineralocorticoid receptor antagonist^[1].

IC₅₀ & Target

Mineralocorticoid receptor^[1]

In Vivo

After single oral administration of Esaxerenone at 0.1, 0.3, 1, and 3 mg/kg, maximum plasma concentration (C_max) and the area under the plasma concentration versus time curve (AUC) are increased with dose. Time to reach the maximum plasma concentration (T_max) of Esaxerenone ranges from 2.0 to 4.5 h. After intravenous administration of Esaxerenone at 0.1, 0.3, 1, and 3 mg/kg, the total body clearance (CL) and distribution volume at steady state (V_ss) are 3.53 to 6.69 mL/min/kg and 1.47 to 2.49 L/kg, respectively, in rats, and 2.79 to 3.69 mL/min/kg and 1.34 to 1.54 L/kg, respectively, in cynomolgus monkeys. Up to 168 h after administration, 3.9% and 91.4% of dosed radioactivity are excreted in rat urine and feces, respectively, and 95.2% in total. In monkeys, the excreted radioactivity up to 168 h is 11.5% in urine, 82.3% in feces, and 93.9% in total^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

466.47

Formula

C₂₂H₂₁F₃N₂O₄S

CAS No.

1632006-28-0

Appearance

Solid

Color

White to light yellow

SMILES

O=C(C1=CN(CCO)C(C2=CC=CC=C2C(F)(F)F)=C1C)NC3=CC=C(S(=O)(C)=O)C=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (214.38 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1438 mL	10.7188 mL	21.4376 mL
5 mM	0.4288 mL	2.1438 mL	4.2875 mL
10 mM	0.2144 mL	1.0719 mL	2.1438 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.46 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.46 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: 2.08 mg/mL (4.46 mM); Clear solution; Need warming

This protocol yields a clear solution of 2.08 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.93%

Select Batch:

Data Sheet (277 KB) SDS (252 KB)

COA (252 KB) HNMR (258 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Yamada M, et al. Pharmacokinetics, distribution, and disposition of esaxerenone, a novel, highly potent and selective non-steroidal mineralocorticoid receptor antagonist, in rats and monkeys. Xenobiotica. 2017 Dec;47(12):1090-1103. [Content Brief]

Animal Administration
^[1]

Esaxerenone dissolved in vehicle is administered orally or intravenously at doses of 0.1, 0.3, 1, and 3?mg/kg to rats (8 weeks old, 285 to 313?g, four animals per group) or to cynomolgus monkeys (3 to 5 years old, 3.37 to 4.48?kg, four animals per group). The blood is collected with heparinized needles and syringes at the designated sample collection times from the cervical veins of the rats and from the femoral veins of the monkeys. Plasma is obtained by centrifugation (4°C, 1710×g, 15?min) and stored at -80?°C before analysis. To rats (6 weeks old, 146 to 154?g, 4 animals), [¹⁴C] Esaxerenone is orally administered at a single dose of 1?mg/kg prepared in vehicle. Urine and feces are collected for the designated periods. For the monkey study, [¹⁴C] Esaxerenone suspended in 0.5% Methylcellulose (MC) is orally administered to cynomolgus monkeys (3 years old, 2.9 to 3.5?kg, three animals) at a single dose of 1?mg/kg. Urine and feces are collected for a designated period up to 168?h post-dose^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

[1]. Yamada M, et al. Pharmacokinetics, distribution, and disposition of esaxerenone, a novel, highly potent and selective non-steroidal mineralocorticoid receptor antagonist, in rats and monkeys. Xenobiotica. 2017 Dec;47(12):1090-1103. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1438 mL	10.7188 mL	21.4376 mL	53.5940 mL
	5 mM	0.4288 mL	2.1438 mL	4.2875 mL	10.7188 mL
	10 mM	0.2144 mL	1.0719 mL	2.1438 mL	5.3594 mL
	15 mM	0.1429 mL	0.7146 mL	1.4292 mL	3.5729 mL
	20 mM	0.1072 mL	0.5359 mL	1.0719 mL	2.6797 mL
	25 mM	0.0858 mL	0.4288 mL	0.8575 mL	2.1438 mL
	30 mM	0.0715 mL	0.3573 mL	0.7146 mL	1.7865 mL
	40 mM	0.0536 mL	0.2680 mL	0.5359 mL	1.3399 mL
	50 mM	0.0429 mL	0.2144 mL	0.4288 mL	1.0719 mL
	60 mM	0.0357 mL	0.1786 mL	0.3573 mL	0.8932 mL
	80 mM	0.0268 mL	0.1340 mL	0.2680 mL	0.6699 mL
	100 mM	0.0214 mL	0.1072 mL	0.2144 mL	0.5359 mL

Esaxerenone Related Classifications

Cardiovascular Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Esaxerenone1632006-28-0CS-3150 XL-550CS3150CS 3150XL550XL 550XL-550Mineralocorticoid ReceptorInhibitorinhibitorinhibit

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Esaxerenone (Synonyms: CS-3150; XL-550)

Customer Review

Esaxerenone Related Antibodies

2 Publications Citing Use of MCE Esaxerenone

Featured Recommendations

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•Related Small Molecules:

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Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Molarity Calculator

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Complete Stock Solution Preparation Table

Esaxerenone Related Classifications

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