Exicorilant |
| Catalog No.GC70442 |
Exicorilant (Cort 125281) est un antagoniste sélectif des récepteurs glucocorticoïdes actifs (RG) par voie orale avec une valeur de ki de 7 nm.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1781244-77-6
Sample solution is provided at 25 µL, 10mM.
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Exicorilant (CORT 125281) reverses corticosterone-mediated GR activity in murine brown adipocytes in vitro[1].
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].
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.
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