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ChemicalBook--->CAS DataBase List--->1781244-77-6

1781244-77-6

1781244-77-6 Structure

1781244-77-6 Structure
IdentificationBack Directory
[Name]

Exicorilant
[CAS]

1781244-77-6
[Synonyms]

CORT-125281
Exicorilant
Methanone, [(4aR,8aS)-1-(4-fluorophenyl)-1,4,5,6,7,8,8a,9-octahydro-6-[(2-methyl-2H-1,2,3-triazol-4-yl)sulfonyl]-4aH-pyrazolo[3,4-g]isoquinolin-4a-yl][4-(trifluoromethyl)-2-pyridinyl]-
[Molecular Formula]

C26H23F4N7O3S
[MOL File]

1781244-77-6.mol
[Molecular Weight]

589.56
Chemical PropertiesBack Directory
[Boiling point ]

719.4±70.0 °C(Predicted)
[density ]

1.59±0.1 g/cm3(Predicted)
[form ]

Solid
[pka]

1.05±0.40(Predicted)
[color ]

Light yellow to yellow
Hazard InformationBack Directory
[Uses]

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].
[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. DOI:10.1021/acs.jmedchem.7b00162
[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. DOI:10.1210/en.2017-00512
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