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 > SR9011 hydrochloride
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:
 
SR9011 hydrochloride
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。
SR9011 hydrochloride图片
CAS NO:2070014-94-5
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
2mg电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
SR9011 hydrochloride 是一种REV-ERBα/β激动剂,作用于 REV-ERBα 和 REV-ERBβ,IC50s 分别为 790 nM 和 560 nM。
生物活性

SR9011 hydrochloride is aREV-ERBα/βagonist withIC50s of 790 nM and 560 nM for REV-ERBα and REV-ERBβ, respectively.

IC50& Target

IC50: 790 nM (Rev-ErbBα), 560 nM (Rev-ErbBβ)[1]

体外研究
(In Vitro)

SR9011 dose-dependently increases the REV-ERB-dependent repressor activity assessed in HEK293 cells expressing a chimeric Gal4 DNA Binding Domain (DBD) - REV-ERB ligand binding domain (LBD) α or β and a Gal4-responsive luciferase reporter (REV-ERBα IC50=790 nM, REV-ERBβ IC50=560 nM). SR9011 potently and efficaciously suppresses transcription in a cotransfection assay using full-length REV-ERBα along with a luciferase reporter driven by theBmal1promoter (SR9011 IC50=620 nM). SR9011 suppresses the expression ofBMAL1 mRNA in HepG2 cells in aREV-ERBα/β-dependent manner[1]SR9011 suppresses proliferation of the breast cancer cell lines regardless of their ER or HER2 status. SR9011 appears to pause the cell cycle of the breast cancer cells prior to M phase. Cyclin A (CCNA2) is identified as a direct target gene of REV-ERB suggesting that suppression of expression of this cyclin by SR9011 may mediate the cell cycle arrest. Treatment with SR9011 results in an increase in cells in the G0/G1phase and a decrease of cells in S and G2/M phase suggesting that activation of REV-ERB may be resulting in decreased transition from G1to S phase and/or from S to G2/M phase[2].

体内研究
(In Vivo)

SR9011 displays reasonable plasma exposure, thus, the expression of REV-ERB responsive genes is examined in the liver of mice treated with various doses of SR9011 for 6-days. Theplasminogen activator inhibitor type 1gene (Serpine1) is a REV-ERB target gene and displays dose-dependent suppression of expression in response to SR9011. Thecholesterol 7α-hydroxylase(Cyp7a1) andsterol response element binding protein(Srepf1) genes have also been shown to be responsive to REV-ERB and are dose-dependently suppressed with increasing amounts of SR9011. After 12 days in D:D conditions mice are injected with a single dose of SR9011 or vehicle at CT6 (peak expression ofRev-erbα). Vehicle injection causes no disruption in circadian locomotor activity. However, administration of a single dose of SR9011 results in loss of locomotor activity during the subject dark phase. Normal activity returns the next circadian cycle, consistent with clearance of the drugs in less than 24h. The SR9011-dependent decrease in wheel running behavior in the mice under constant darkness conditions is dose-dependent and that the potency (ED50=56 mg/kg) is similar to the potency of SR9011-mediated suppression of a REV-ERB responsive gene,Srebf1, in vivo (ED50=67mg/kg)[1].

分子量

515.50

性状

Solid

Formula

C23H32Cl2N4O3S

CAS 号

2070014-94-5

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)

溶解性数据
In Vitro: 

DMSO : ≥ 32 mg/mL(62.08 mM)

H2O :< 0.1 mg/mL (ultrasonic;warming;heat to 60℃)(insoluble)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.9399 mL9.6993 mL19.3986 mL
5 mM0.3880 mL1.9399 mL3.8797 mL
10 mM0.1940 mL0.9699 mL1.9399 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。