1. Metabolic Enzyme/Protease
  2. Mineralocorticoid Receptor

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

Cat. No.: HY-100471 Purity: 99.65%
Handling Instructions

Esaxerenone is a novel, highly potent and selective non-steroidal mineralocorticoid receptor antagonist.

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

Esaxerenone Chemical Structure

Esaxerenone Chemical Structure

CAS No. : 1632006-28-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 406 In-stock
Estimated Time of Arrival: December 31
1 mg USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 396 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Esaxerenone is a novel, highly potent and selective non-steroidal mineralocorticoid receptor antagonist.

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 (Cmax) and the area under the plasma concentration versus time curve (AUC) are increased with dose. Time to reach the maximum plasma concentration (Tmax) 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 (Vss) 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].

Clinical Trial
Solvent & Solubility
In Vitro: 

10 mM in 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
*Please refer to the solubility information to select the appropriate solvent.
References
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
Molecular Weight

466.47

Formula

C₂₂H₂₁F₃N₂O₄S

CAS No.

1632006-28-0

SMILES

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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.65%

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Product Name:
Esaxerenone
Cat. No.:
HY-100471
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Esaxerenone

Cat. No.: HY-100471