Exicorilant |
Catalog No.GC70442 |
Exicorilant (CORT 125281)는 선택적 경구 활성 당피질 호르몬 수용체(GR) 옹색제로서 Ki 값은 7nM입니다.
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.
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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