MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

SR9011 hydrochloride

CAS No. : 2070014-94-5

MCE 站：SR9011 hydrochloride

产品活性：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。

研究领域：Autophagy

作用靶点：Autophagy

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 the Bmal1 promoter (SR9011 IC₅₀=620 nM). SR9011 suppresses the expression ofBMAL1 mRNA in HepG2 cells in a REV-ERBα/β-dependent manner 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/G₁ phase and a decrease of cells in S and G₂/M phase suggesting that activation of REV-ERB may be resulting in decreased transition from G₁ to S phase and/or from S to G₂/M phase.

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. 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 (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).

相关产品：Bioactive Compound Library Plus  |  Anti-Cancer Compound Library  |  Autophagy Compound Library  |  Anti-Breast Cancer Compound Library  |  MG-132  |  Rapamycin  |  3-Methyladenine  |  Cisplatin  |  LY294002  |  Doxorubicin hydrochloride  |  Bafilomycin A1  |  Paclitaxel  |  Cycloheximide  |  Venetoclax  |  CHIR-99021  |  SB 203580  |  Chloroquine  |  Deferoxamine mesylate  |  Resatorvid  |  SP600125  |  Dexamethasone  |  Bortezomib  |  Metformin hydrochloride  |  Tamoxifen  |  Forskolin  |  Oxaliplatin  |  Dorsomorphin  |  Gemcitabine  |  Necrostatin-1  |  PD98059  |  U0126-EtOH  |  Verteporfin  |  Actinomycin D

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。