Dazucorilant|1496508-34-9|(CORT113176)-陌孚医药/Medlife

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Dazucorilant (Synonyms: CORT113176)

目录号: PL03312 纯度: ≥98%

CAS No. :1496508-34-9

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PL03312-50mg	50mg	询价	询价
PL03312-100mg	100mg	询价	询价

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中文名称	Dazucorilant
英文名称	Dazucorilant
英文别名	Dazucorilant;HR4RD5RBJ6;Dazucorilant [INN];BDBM50265674;(R)-(1-(4-fluorophenyl)-6-((4-(trifluoromethyl)phenyl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(pyridin-2-yl)methanone;Methanone, ((4aR)-1-(4-fluorophenyl)-1,4,5,6,7,8-hexahydro-6-((4-(trifluoromethyl)phenyl)sulfonyl)-4ah-pyrazolo(3,4-g)isoquinolin-4a-yl)-2-pyridinyl-;Unii-HR4RD5rbj6
Cas No.	1496508-34-9
分子式	C₂₉H₂₂F₄N₄O₃S
分子量	582.57
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

Dazucorilant (CORT113176) 是一种非甾体糖皮质激素受体 (GR) 调节剂，在体外其 K_i 值 <1 nM。Dazucorilant 可用于神经系统疾病的研究。

生物活性

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

性状

Solid

IC50 & Target[1][2]

体外研究(In Vitro)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Dazucorilant (30 mg/kg/day; s.c.) makes mice show reversed abnormalities of motoneurons and down-regulated proinflammatory mediators and glial reactivity.
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. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[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.

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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