| Bioactivity | 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]. | ||||||||||||
| Target | Ki: 7 nM (GR). | ||||||||||||
| Invitro | Exicorilant (CORT 125281) reverses corticosterone-mediated GR activity in murine brown adipocytes in vitro[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Exicorilant 相关抗体: | ||||||||||||
| 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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: | ||||||||||||
| CAS | 1781244-77-6 | ||||||||||||
| Formula | C26H23F4N7O3S | ||||||||||||
| Molar Mass | 589.56 | ||||||||||||
| Appearance | 固体 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |
Exicorilant
CAS: 1781244-77-6 F: C26H23F4N7O3S W: 589.56
Exicorilant (CORT 125281) is a selective and oral active glucocorticoid receptor (GR) antagonist, with a Ki value of 7 n
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