1. GPCR/G Protein
  2. Glucocorticoid Receptor
  3. Exicorilant

Exicorilant (Synonyms: CORT 125281)

Cat. No.: HY-117880 Purity: 99.89%
Handling Instructions

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

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 454 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
25 mg USD 990 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2250 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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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].

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].

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%).
Clinical Trial
Molecular Weight

589.56

Formula

C₂₆H₂₃F₄N₇O₃S

CAS No.

1781244-77-6

SMILES

O=C([[email protected]]12CC3=C(N(C4=CC=C(F)C=C4)N=C3)C[[email protected]]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)

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
10 mM 0.1696 mL 0.8481 mL 1.6962 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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Keywords:

ExicorilantCORT 125281CORT125281CORT-125281Glucocorticoid ReceptorInhibitorinhibitorinhibit

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Product name:
Exicorilant
Cat. No.:
HY-117880
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