Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Dazucorilant (CORT113176) is a non-steroidal glucocorticoid receptor (GR) modulator characterized by its high affinity and selectivity. With an impressive K i value of <1 nM in vitro, Dazucorilant proves to be an exceptional compound for investigating neurological disorders.
产品描述 | Dazucorilant (CORT113176) is a non-steroidal glucocorticoid receptor (GR) modulator characterized by its high affinity and selectivity. With an impressive K i value of <1 nM in vitro, Dazucorilant proves to be an exceptional compound for investigating neurological disorders. |
体外活性 | 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]. |
体内活性 | 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]. Animal Model: Wobbler mice (five-month-old)[1]Dosage: 30 mg/kg/day Administration: S.c. Result: Wobbler mice showed reversed abnormalities of motoneurons and down-regulated proinflammatory mediators and glial reactivity. Animal Model: Adult SD male rats[2]Dosage: 5, 10 or 20 mg/kg Administration: I.p. Result: Reversed hippocampal amyloid-β peptide generation, neuroinflammation and apoptotic processes, restored the hippocampal levels of synaptic markers, reestablished basal plasma levels of glucocorticoids and improved cognitive function at a dose of 10 mg/kg. |
别名 | CORT113176 |
分子量 | 582.57 |
分子式 | C29H22F4N4O3S |
CAS No. | 1496508-34-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Dazucorilant 1496508-34-9 CORT113176 CORT 113176 CORT-113176 Inhibitor inhibitor inhibit