Dazucorilant

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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。

CAS NO:

1496508-34-9

CORT113176

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-steroidalglucocorticoid receptor(GR) modulator with aK_ivalue ＜1 nM in vitro. Dazucorilant can be used for the research of neurological disorders^[1]^[2].

IC₅₀& Target

GR^[1]

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^[3].

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^[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.

Clinical Trial

分子量

582.57

性状

Solid

Formula

C₂₉H₂₂F₄N₄O₃S

CAS 号

1496508-34-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

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