2. Immunology/Inflammation Vitamin D Related/Nuclear Receptor
  3. Glucocorticoid Receptor
  4. Exicorilant

Exicorilant  (Synonyms: CORT 125281)

Cat. No.: HY-117880 Purity: 98.28%
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Exicorilant (CORT 125281) is a selective and oral active glucocorticoid receptor (GR) antagonist, with a Ki value of 7 nM. Exicorilant (CORT 125281) has potential to overcome adiposity, glucose intolerance and dyslipidaemia.

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

Exicorilant Chemical Structure

Exicorilant Chemical Structure

CAS No. : 1781244-77-6

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Solid + Solvent
10 mM * 1 mL in DMSO
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 USD 454 In-stock
Solution
10 mM * 1 mL in DMSO USD 454 In-stock
Solid
5 mg USD 350 In-stock
10 mg USD 550 In-stock
25 mg USD 990 In-stock
50 mg USD 1650 In-stock
100 mg USD 2250 In-stock
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Based on 1 publication(s) in Google Scholar

Exicorilant Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

Exicorilant (CORT 125281) is a selective and oral active glucocorticoid receptor (GR) antagonist, with a Ki value of 7 nM[1]. Exicorilant (CORT 125281) has potential to overcome adiposity, glucose intolerance and dyslipidaemia[2].

IC50 & Target

Ki: 7 nM (GR)[1].
In Vitro

Exicorilant (CORT 125281) reverses corticosterone-mediated GR activity in murine brown adipocytes in vitro[1].

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

Exicorilant Related Antibodies
In Vivo

Exicorilant (CORT 125281) reduces body weight, fat mass and plasma lipids in HFD-fed mice[2].
Exicorilant (CORT 125281) (6, 20 or 60 mg/kg/d, for 3 weeks in mice) at different dosages reduce body weight, fat mass, plasma TG, cholesterol and FFA in a dose-dependent manner, with no effect on lean mass[2].

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

Animal Model: Ten-week old male C57BL/6J mice HFD-fed[2].
Dosage: 6, 20, 60 mg/kg.
Administration: Orally mixed with food daily for 3 weeks.
Result: Reduced HFD-induced body weight gain with approximately 10% for CORT125281 at d21.
Significantly lowered plasma TG (-56%) and cholesterol levels (-30%).
Molecular Weight

589.56

Formula

C26H23F4N7O3S
CAS No.
Appearance

Solid

SMILES

O=C([C@]12CC3=C(N(C4=CC=C(F)C=C4)N=C3)C[C@]1([H])CCN(S(=O)(C5=NN(C)N=C5)=O)C2)C6=NC=CC(C(F)(F)F)=C6
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (424.05 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 1.6962 mL 8.4809 mL 16.9618 mL
5 mM 0.3392 mL 1.6962 mL 3.3924 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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 (3.53 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% Corn Oil

    Solubility: ≥ 2.08 mg/mL (3.53 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). 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)

g

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
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6962 mL 8.4809 mL 16.9618 mL 42.4045 mL
5 mM 0.3392 mL 1.6962 mL 3.3924 mL 8.4809 mL
10 mM 0.1696 mL 0.8481 mL 1.6962 mL 4.2405 mL
15 mM 0.1131 mL 0.5654 mL 1.1308 mL 2.8270 mL
20 mM 0.0848 mL 0.4240 mL 0.8481 mL 2.1202 mL
25 mM 0.0678 mL 0.3392 mL 0.6785 mL 1.6962 mL
30 mM 0.0565 mL 0.2827 mL 0.5654 mL 1.4135 mL
40 mM 0.0424 mL 0.2120 mL 0.4240 mL 1.0601 mL
50 mM 0.0339 mL 0.1696 mL 0.3392 mL 0.8481 mL
60 mM 0.0283 mL 0.1413 mL 0.2827 mL 0.7067 mL
80 mM 0.0212 mL 0.1060 mL 0.2120 mL 0.5301 mL
100 mM 0.0170 mL 0.0848 mL 0.1696 mL 0.4240 mL
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Exicorilant Related Classifications

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:

Exicorilant1781244-77-6CORT 125281CORT125281CORT-125281Glucocorticoid ReceptorInhibitorinhibitorinhibit

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