產(chǎn)品目錄

規(guī)格	5mg 10mg 25mg 100mg
CAS	1379686-30-2
別名	N/A
化學(xué)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
儲(chǔ)存條件	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

產(chǎn)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.

特別提醒：

1. 本產(chǎn)品僅供科研使用。請(qǐng)勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請(qǐng)勿存放于普通住宅區(qū)。

2. 為了您的安全和健康，請(qǐng)穿好實(shí)驗(yàn)服并佩戴一次性手套和口罩操作。

原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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