Dazucorilant (Synonyms: CORT113176) |
カタログ番号GC64330 |
ダズコリラント (CORT113176) は、選択的で高親和性の非ステロイド性グルココルチコイド受容体 (GR) モジュレーターであり、in vitro での Ki 値は <1 nM です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1496508-34-9
Sample solution is provided at 25 µL, 10mM.
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.
Average Rating: 5
(Based on Reviews and 19 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *