Esaxerenone
Based on 2 publication(s) in Google Scholar
Esaxerenone (CS-3150) is a highly potent and selective non-steroidal mineralocorticoid receptor antagonist.
For research use only. We do not sell to patients.
- Purity: 99.93%
- CAS No.: 1632006-28-0
- Formula: C22H21F3N2O4S
- Molecular Weight:466.47
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Esaxerenone
More
Biological Activity
Mineralocorticoid receptor[1]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1632006-28-0
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Appearance Solid
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Molecular Weight 466.47
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Formula C22H21F3N2O4S
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Color White to light yellow
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SMILES
O=C(C1=CN(CCO)C(C2=CC=CC=C2C(F)(F)F)=C1C)NC3=CC=C(S(=O)(C)=O)C=C3
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Synonyms
CS-3150; XL-550
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Biomedicines
Effective Accentuation of Voltage-Gated Sodium Current Caused by Apocynin (4'-Hydroxy-3'-methoxyacetophenone), a Known NADPH-Oxidase Inhibitor. [Abstract]2021 Sep 3;9(9):1146. PMID: 34572332 -
Biomedicines
Characterization of Direct Perturbations on Voltage-Gated Sodium Current by Esaxerenone, a Nonsteroidal Mineralocorticoid Receptor Blocker. [Abstract]2021 May 13;9(5):549. PMID: 34068333
Solvent & Solubility
DMSO : ≥ 100 mg/mL (214.38 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.36 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.36 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| 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
HY-100471 Related Classifications
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