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SR9011 hydrochloride

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产品编号 T39473Cas号 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.

SR9011 hydrochloride

SR9011 hydrochloride

Rating icon 还可以
产品编号 T39473Cas号 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.

规格价格库存数量
2 mg
¥ 1,150
5日内发货
5 mg
¥ 2,320
5日内发货
25 mg
¥ 9,540
1-2周
50 mg
¥ 12,400
1-2周
100 mg
¥ 17,400
1-2周
1 mL x 10 mM (in DMSO)
¥ 2,760
5日内发货
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TargetMol 的所有产品仅用作科学研究或药证申报,不能被用于人体,我们不向个人提供产品和服务。请您遵守承诺用途,不得违反法律法规规定用于任何其他用途。
实验操作小课堂
常见问题解答
如何选择合适的溶剂?
常用的溶剂包括DMSO、水、乙醇等。建议您根据抑制剂给出的溶解度参考,选择合适的溶剂。如果该抑制剂可以溶于DMSO,建议使用没有吸潮新开封的 DMSO,如果有潮气污染,很容易带来抑制剂降解或难溶的问题。如果该抑制剂可以溶于水,建议您根据实验类型选择无菌水、生理盐水、无菌 PBS 、培养基等作为溶剂。
是否能直接用缓冲液对抑制剂 DMSO 母液做梯度稀释?
大部分情况下,都是可以溶解的。但有时,有机试剂直接加入水相介质时会析出。建议将抑制剂先以DMSO做梯度稀释,再将经过稀释的抑制剂加入缓冲液或细胞培养基。有些抑制剂甚至只有在其工作浓度下才能溶于水相。 比如细胞实验中希望终浓度为 1 μM 的话,可以把 10 mM 的 DMSO 母液用 DMSO 稀释到 1 mM,再吸 2 μL 加入到 2 mL 的生理盐水/PBS/细胞培液,终浓度即为 1 μM。 为避免药物析出,稀释前,可将母液和培养基 37℃ 预热,避免温度低造成严重析出。若稀释过程中出现化合物析出的情况,建议您采用超声加热的方法使其复溶。
溶解度中写的“< 1 mg/mL refers to the slightly soluble or insoluble ”是什么意思?
这句话指的是,如果溶解度 < 1 mg/mL,那我们就认为它是微溶或不溶的,这是针对写的“DMSO:Insoluble”或“DMSO:slightly soluble”这类化合物的。
期货产品没有纯度啊?这个纯度在哪里看
期货产品的话,是没有纯度信息,也没有质检信息的。有了现货之后我们会进行质检,测出试剂的纯度和结构等相关信息,并且展示在官网的活性描述上方。
超声应使用什么样的频率?
频率建议使用常规的超声清洗频率即可,一般在20 kHz - 100 kHz。
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产品介绍

生物活性
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-ErbBα:790 nM (IC50), Rev-ErbBβ:560 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].
化学信息
分子量515.49
分子式C23H32Cl2N4O3S
CAS No.2070014-94-5
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

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:
TargetMol | Animal experiments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 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent 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 μLDMSOTargetMol | reagent ( 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:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

剂量转换

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