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Dazucorilant
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Dazucorilant图片
CAS NO:1496508-34-9
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品介绍
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。
Cas No.1496508-34-9
别名CORT113176
分子式C29H22F4N4O3S
分子量582.57
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.