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

SR9011 hydrochloride 是一種 REV-ERBα/β 激動劑，作用于 REV-ERBα 和 REV-ERBβ，IC50s 分別為 790 nM 和 560 nM。

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SR9011 hydrochloride Chemical Structure

SR9011 hydrochloride Chemical Structure

CAS No. : 2070014-94-5

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥1815
In-stock
2 mg ￥900
In-stock
5 mg ￥1600
In-stock
10 mg ￥2600
In-stock
50 mg   詢價(jià)  
100 mg   詢價(jià)  

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Customer Review

Other Forms of SR9011 hydrochloride:

    SR9011 hydrochloride purchased from MCE. 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

    • 生物活性

    • 實(shí)驗(yàn)參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    SR9011 hydrochloride 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]
    體外研究
    (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 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].

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

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

    515.50

    Formula

    C23H32Cl2N4O3S
    CAS 號
    性狀

    固體

    顏色

    Light yellow to brown

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

    DMSO 中的溶解度 : ≥ 32 mg/mL (62.08 mM; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

    H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

    * "≥" means soluble, but saturation unknown.

    配制儲備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 1.9399 mL 9.6993 mL 19.3986 mL
    5 mM 0.3880 mL 1.9399 mL 3.8797 mL
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲存時(shí)，請?jiān)?個(gè)月內(nèi)使用，-20°C儲存時(shí)，請?jiān)?個(gè)月內(nèi)使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動物溶解方案計(jì)算器
    請輸入動物實(shí)驗(yàn)的基本信息：

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    只
    由于實(shí)驗(yàn)過程有損耗，建議您多配一只動物的量
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    純度 & 產(chǎn)品資料

    純度: 99.39%

    參考文獻(xiàn)
    Cell Assay
    [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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    參考文獻(xiàn)

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲存時(shí)，請?jiān)?個(gè)月內(nèi)使用，-20°C儲存時(shí)，請?jiān)?個(gè)月內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9399 mL 9.6993 mL 19.3986 mL 48.4966 mL
    5 mM 0.3880 mL 1.9399 mL 3.8797 mL 9.6993 mL
    10 mM 0.1940 mL 0.9699 mL 1.9399 mL 4.8497 mL
    15 mM 0.1293 mL 0.6466 mL 1.2932 mL 3.2331 mL
    20 mM 0.0970 mL 0.4850 mL 0.9699 mL 2.4248 mL
    25 mM 0.0776 mL 0.3880 mL 0.7759 mL 1.9399 mL
    30 mM 0.0647 mL 0.3233 mL 0.6466 mL 1.6166 mL
    40 mM 0.0485 mL 0.2425 mL 0.4850 mL 1.2124 mL
    50 mM 0.0388 mL 0.1940 mL 0.3880 mL 0.9699 mL
    60 mM 0.0323 mL 0.1617 mL 0.3233 mL 0.8083 mL
    Help & FAQs
    • 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.

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    產(chǎn)品名稱：
    SR9011 hydrochloride
    目錄號：
    HY-16988A
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