Exicorilant (CORT 125281) | Glucocorticoid Receptor Antagonist
国际站:Exicorilant (CORT 125281) | Glucocorticoid Receptor Antagonist
CAS:1781244-77-6
纯度:98.28%
分子量:589.56
Formula:C26H23F4N7O3S
运输条件:Room temperature in continental US; may vary elsewhere.
储存方式:
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
产品活性:Exicorilant (CORT 125281) 是选择性的、并具有口服活性的糖皮质激素受体 (GR) 的拮抗剂,其 Ki 值为 7 nM。Exicorilant (CORT 125281) 具有克服肥胖、葡萄糖不耐受和血脂异常的潜能。
生物活性:Exicorilant (CORT 125281)是一种选择性口服活性糖皮质激素受体(GR)拮抗剂,Ki值为7 nM[1]。Exicorilant (CORT 125281)具有克服肥胖、葡萄糖耐受不良和血脂异常的潜力[2]。
体外:Exicorilant (CORT 125281)在体外逆转皮质酮介导的小鼠棕色脂肪细胞GR活性[1]。
体内:
Exicorilant (CORT 125281)可降低hfd喂养小鼠的体重、脂肪量和血脂[2]。
Exicorilant (CORT 125281)(6、20或60 mg/kg/d,小鼠3周)以不同剂量降低体重、脂肪量、血浆TG、胆固醇和FFA,呈剂量依赖性,对瘦质量无影响[2]。
参考文献:
[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.