2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. REV-ERB
  4. SR9011

SR9011 is a REV-ERBα/β agonist with IC50s of 790 nM and 560 nM for REV-ERBα and REV-ERBβ, respectively.

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CAS 番号 : 1379686-29-9

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 200 在庫あり
Solution
10 mM * 1 mL in DMSO USD 200 在庫あり
Solid
2 mg $95 在庫あり
5 mg $190 在庫あり
10 mg $332 在庫あり
25 mg $590 在庫あり
50 mg $900 在庫あり
100 mg $1350 在庫あり
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カスタマーレビュー

Based on 8 publication(s) in Google Scholar

Other Forms of SR9011:

SR9011 関連抗体

Top Publications Citing Use of Products

    SR9011 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2019 Jan;40(1):26-34.  [Abstract]

    BV2 cells are pretreated with different doses of SR9011 (0-10 μM) for 4 h and then exposed to LPS (100 ng/mL) for 12 h. Cell lysates are analyzed by Western blot for iNOS, COX-2, and GAPDH. The relative band intensities of iNOS and COX-2 to GAPDH are analyzed

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    製品説明

    SR9011 is a REV-ERBα/β agonist with IC50s 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]
    Cellular Effect
    Cell Line Type Value Description References
    HEK293 IC50
    560 nM
    Compound: SR9011
    Increased REV-ERB-beta LBD dependent repressor activity in HEK293 cell reporter assay
    Increased REV-ERB-beta LBD dependent repressor activity in HEK293 cell reporter assay
    		[PMID: 22460951]
    HEK293 IC50
    620 nM
    Compound: SR9011
    REV-ERB-alpha mediated transcriptional suppression at Bmal1 promoter in HEK293 cell reporter assay
    REV-ERB-alpha mediated transcriptional suppression at Bmal1 promoter in HEK293 cell reporter assay
    		[PMID: 22460951]
    HEK293 IC50
    790 nM
    Compound: SR9011
    Increased REV-ERB-alpha LBD dependent repressor activity in HEK293 cell reporter assay
    Increased REV-ERB-alpha LBD dependent repressor activity in HEK293 cell reporter assay
    		[PMID: 22460951]
    体外実験

    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[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/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[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    SR9011 関連抗体
    体内実験

    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)[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    分子量

    479.04

    分子式

    C23H31ClN4O3S
    CAS 番号
    Appearance

    Solid

    Color

    Off-white to yellow

    SMILES

    O=C(N1CC(CN(CC2=CC=C(Cl)C=C2)CC3=CC=C([N+]([O-])=O)S3)CC1)NCCCCC
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : ≥ 43 mg/mL (89.76 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.0875 mL 10.4375 mL 20.8751 mL
    5 mM 0.4175 mL 2.0875 mL 4.1750 mL
    10 mM 0.2088 mL 1.0438 mL 2.0875 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

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    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.22 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (5.22 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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    Please enter your animal formula composition:
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    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 99.78%

    COA (250 KB) LCMS (94 KB)

    取扱説明書 (2659 KB)
    参考文献
    細胞実験
    [2]

    MCF10A, MDA-MB-231, MCF-7, MDA-MB-361, SKBR3, BT474 cells are plated in 6-well plates one day before treatment. The MTT cell proliferation assays are performed. Briefly, 3×103 to 5 × 103 cells per well are plated in 96-well plates. Twenty-four hours later, cells are treated with SR9011 (0, 2, 4, 6, 8 and 10 μM) or DMSO. Seventy-two hours after treatment, the cells are labeled with 1.2 mM MTT and incubated for 4 hours. DMSO is then added and readings are taken on a plate reader at 540 nm[2].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [1]

    Mice[1]
    For circadian gene expression experiments male C57BL6 mice (8-10 weeks of age) are either maintained on a L:D (12h:12h) cycle or on constant darkness. At circadian time (CT) 0 animals are administered a single dose of 100 mg/kg SR9011 (i.p.) and groups of animals (n=6) are sacrificed at CT0, CT6, CT12 and CT18. Gene expression is determined by real time QPCR.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.0875 mL 10.4375 mL 20.8751 mL 52.1877 mL
    5 mM 0.4175 mL 2.0875 mL 4.1750 mL 10.4375 mL
    10 mM 0.2088 mL 1.0438 mL 2.0875 mL 5.2188 mL
    15 mM 0.1392 mL 0.6958 mL 1.3917 mL 3.4792 mL
    20 mM 0.1044 mL 0.5219 mL 1.0438 mL 2.6094 mL
    25 mM 0.0835 mL 0.4175 mL 0.8350 mL 2.0875 mL
    30 mM 0.0696 mL 0.3479 mL 0.6958 mL 1.7396 mL
    40 mM 0.0522 mL 0.2609 mL 0.5219 mL 1.3047 mL
    50 mM 0.0418 mL 0.2088 mL 0.4175 mL 1.0438 mL
    60 mM 0.0348 mL 0.1740 mL 0.3479 mL 0.8698 mL
    80 mM 0.0261 mL 0.1305 mL 0.2609 mL 0.6523 mL
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    SR9011 Related Classifications

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    SR90111379686-29-9SR 9011SR-9011REV-ERBInhibitorinhibitorinhibit

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    製品名:
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    製品番号:
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