Exicorilant

Modify Date: 2025-08-25 09:37:02

Exicorilant Structure
Exicorilant structure
Common Name Exicorilant
CAS Number 1781244-77-6 Molecular Weight 589.56
Density N/A Boiling Point N/A
Molecular Formula C26H23F4N7O3S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Exicorilant


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].

 Names

Name Exicorilant

 Exicorilant Biological Activity

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].
Related Catalog
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%).
References

[1]. Hunt HJ, et al. Identification of the Clinical Candidate (R)-(1-(4-Fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone (CORT125134): A Selective Glucocorticoid Receptor (GR) Antagonist. J Med Chem. 2017 Apr 27;60(8):3405-3421.

[2]. Kroon J, et al. Selective Glucocorticoid Receptor Antagonist CORT125281 Activates Brown Adipose Tissue and Alters Lipid Distribution in Male Mice. Endocrinology. 2018 Jan 1;159(1):535-546.

 Chemical & Physical Properties

Molecular Formula C26H23F4N7O3S
Molecular Weight 589.56
The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.