您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > Dazucorilant
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
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
50mg电议
100mg电议

产品名称
CORT113176
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。
生物活性

Dazucorilant (CORT113176) is a selective and high affinity non-steroidalglucocorticoid receptor(GR) modulator with aKivalue <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)