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抑制剂 > 泛素化/蛋白酶体 > SR9009
产品名称:
SR9009
型号:
CS-01Y73909
生产地址
进口、国产
产品价格
电议
产品简介
质量保证、价格优惠
产品详情

一、概述:

化学性质:                                                                                                             

规格

5mg 10mg 25mg 100mg

CAS

1379686-30-2

别名

N/A

化学名

ethyl 3-(((4-chlorobenzyl)((5-nitrothiophen-2-yl)methyl)amino)methyl)pyrrolidine-1-carboxylate

分子式

C20H24ClN3O4S

分子量

437.94

溶解度

43.8mg/mL in DMSO

储存条件

Store at -20°C

General tips

For obtaining a higher solubility , please warm the tube at 37 and shake it in the ultrasonic bath for a while.

Shipping Condition

Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

 

产品描述:                                                                                                            

IC50: 670 nM for REV-ERB-α and 800 nM for REV-ERB-β

SR9009, also known as Stenabolic, is a research drug as agonist of REV-ERB.

REV-ERB-α and REV-ERB-β, two nuclear receptors, have a critical role in regulating the expression of core clock proteins driving rhythms in activity and metabolism.

In vitro: Both SR9009 and its analog SR9011 could dose-dependently increase the REV-ERB-dependent repressor activity assessed in HEK293 cells expressing a chimaeric Gal4 DNA binding domain: REV-ERB ligand binding domain α or β and a Gal4-responsive luciferase reporter. In addition, SR9009 was found to be able to suppress BMAL1 messenger RNA expression in HepG2 cells in a REV-ERB-α/β-dependent manner [1].

In vivo: Mice were treated with a single dose of SR9009, SR9011 or vehicle at circadian time 6 (CT6 (6h after lights on) after 12 days in D/D conditions showing peak expression of Rev-erb-α. Results showed that vehicle injection caused no disruption in circadian locomotor activity. In contrast, administration of a single dose of either SR9009 or SR9011 led to the loss of locomotor activity during the subject dark phase. In addition, the normal activity returned the next circadian cycle, which was consistent with clearance of the drugs in less than 24h [1].

Clinical trial: Up to now, SR9009 is still in the preclinical development stage.

特别提醒:                                                                                                              

1. 本产品仅供科研使用。请勿用于医药、临床诊断或治疗,食品及化妆品等用途。请勿存放于普通住宅区。

2. 为了您的安全和健康,请穿好实验服并佩戴一次性手套和口罩操作。

标签:SR9009 

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