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SR9011 hydrochloride

产品编号 T39473 CAS 2070014-94-5

SR9011 hydrochloride is a REV-ERBα/β agonist, exhibiting an IC50 value of 790 nM for REV-ERBα and 560 nM for REV-ERBβ.

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SR9011 hydrochloride, CAS 2070014-94-5

规格	价格/CNY	货期
2 mg	￥ 1,150	5日内发货
5 mg	￥ 2,320	5日内发货
25 mg	￥ 9,540	6-8周
50 mg	￥ 12,400	6-8周
100 mg	￥ 17,400	6-8周
1 mL * 10 mM (in DMSO)	￥ 2,760	5日内发货

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SR9011 hydrochloride 的其他形式现货产品:

SR9011

其他形式的 SR9011 hydrochloride:

SR9011
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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	SR9011 hydrochloride is a REV-ERBα/β agonist, exhibiting an IC50 value of 790 nM for REV-ERBα and 560 nM for REV-ERBβ.
靶点活性	Rev-ErbBβ:560 nM (IC50), Rev-ErbBα:790 nM (IC50)
体外活性	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 IC 50 =790 nM, REV-ERBβ IC 50 =560 nM). SR9011 potently and efficaciously suppresses transcription in a cotransfection assay using full-length REV-ERBα along with a luciferase reporter driven by the Bmal1 promoter (SR9011 IC 50 =620 nM). SR9011 suppresses the expression ofBMAL1 mRNA in HepG2 cells in a REV-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 G 0 /G 1 phase and a decrease of cells in S and G 2 /M phase suggesting that activation of REV-ERB may be resulting in decreased transition from G 1 to S phase and/or from S to G 2 /M phase[2].
体内活性	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. The plasminogen activator inhibitor type 1 gene ( Serpine1 ) is a REV-ERB target gene and displays dose-dependent suppression of expression in response to SR9011. The cholesterol 7α-hydroxylase ( Cyp7a1 ) and sterol 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 of Rev-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 (ED 50 =56 mg/kg) is similar to the potency of SR9011-mediated suppression of a REV-ERB responsive gene, Srebf1 , in vivo (ED 50 =67mg/kg)[1].

分子量	515.49
分子式	C23H32Cl2N4O3S
CAS No.	2070014-94-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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参考文献

1. Solt LA, et al. Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. Nature. 2012 Mar 29;485(7396):62-8. 2. Wang Y, et al. Anti-proliferative actions of a synthetic REV-ERBα/β agonist in breast cancer cells. Biochem Pharmacol. 2015 Aug 15;96(4):315-22.

剂量换算

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体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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