Dazucorilant (CORT113176) 是一种非甾体糖皮质激素受体 (GR) 调节剂，在体外其 Ki 值<1 nm。dazucorilant 可用于神经系统疾病的研究。
货号:ajcx37404
CAS:1496508-34-9
分子式:C29H22F4N4O3S
分子量：582.57
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Dazucorilant (CORT113176) is a selective and high affinity non-steroidal glucocorticoid receptor (GR) modulator with a Ki value<1 nM in vitro. Dazucorilant can be used for the research of neurological disorders[1][2].

In HepG2 human cells or in human hepatocytes, Dazucorilant acts as full antagonist since it is able to prevent the dexamethasone-induced increase in TAT activity and to induce non-measurable agonist activity in the absence of dexamethasone[3].

Dazucorilant (30 mg/kg/day; s.c.) makes mice show reversed abnormalities of motoneurons and down-regulated proinflammatory mediators and glial reactivity[1]. Dazucorilant (5, 10 or 20 mg/kg; i.p.) reverses hippocampal amyloid-β peptide generation, neuroinflammation and apoptotic processes, restores the hippocampal levels of synaptic markers, reestablishes basal plasma levels of glucocorticoids and improves cognitive function at a dose of 10 mg/kg[2].

[1]. Meyer M, et al. The Selective Glucocorticoid Receptor Modulator Cort 113176 Reduces Neurodegeneration and Neuroinflammation in Wobbler Mice Spinal Cord. Neuroscience. 2018;384:384-396.
[2]. Pineau F, et al. New selective glucocorticoid receptor modulators reverse amyloid-β peptide-induced hippocampus toxicity. Neurobiol Aging. 2016;45:109-122.
[3]. Canet G, et al. Central Role of Glucocorticoid Receptors in Alzheimer’s Disease and Depression. Front Neurosci. 2018;12:739. Published 2018 Oct 16.