DC Chemicals Limited
China
Product Name: Exicorilant
Price: $Inquiry/100mg $Inquiry/250mg $Inquiry/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

1781244-77-6

1781244-77-6 structure

Name: Exicorilant
Chemical Name: Exicorilant
CAS Number: 1781244-77-6
Molecular Formula: C₂₆H₂₃F₄N₇O₃S
Molecular Weight: 589.56
Catalog: Signaling Pathways GPCR/G Protein Glucocorticoid Receptor
Create Date: 2019-06-02 12:05:56
Modify Date: 2024-01-16 17:39:07
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].

Name	Exicorilant

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	Research Areas >> Metabolic Disease Signaling Pathways >> GPCR/G Protein >> Glucocorticoid Receptor
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.

Molecular Formula	C₂₆H₂₃F₄N₇O₃S
Molecular Weight	589.56

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