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  2. Autophagy
  3. Autophagy
  4. SR9009

SR9009 是 REV-ERBα/β 激動(dòng)劑，作用 REV-ERBα 和 REV-ERBβ 的 IC50 分別為 670 nM 和 800 nM。

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SR9009 Chemical Structure

SR9009 Chemical Structure

CAS No. : 1379686-30-2

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3.  試用裝只面向終端客戶。

規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥880
In-stock
1 mg ￥266
In-stock
5 mg ￥800
In-stock
10 mg ￥1100
In-stock
25 mg ￥1700
In-stock
50 mg ￥3100
In-stock
100 mg ￥5100
In-stock
200 mg   詢價(jià)  
500 mg   詢價(jià)  

* Please select Quantity before adding items.

Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 29 篇科研文獻(xiàn)

WB
Cell Viability Assay

    SR9009 purchased from MCE. Usage Cited in: Cell Death Dis. 2022 Nov 10;13(11):949.  [Abstract]

    SR9009 (0-50 μM; 48 h) markedly inhibits 22RV1, PC3 and DU145 cell viability in a dose-dependent manner but had no impact on RWPE-1 cells.

    SR9009 purchased from MCE. Usage Cited in: Chemosphere. 2021 Jan;263:128020.  [Abstract]

    SR9009 administration remarkably increases the protein expression levels of NR1D1 at both 24 and 48 h, while attenuating the protein expression levels of BMAL1. The protein expression levels of StAR are also elevated at 24 h.

    SR9009 purchased from MCE. Usage Cited in: Nat Commun. 2018 Oct 12;9(1):4246.  [Abstract]

    Western blotting of peritoneal macrophages (PMs) after co-treatment of SR9009 (for 12?h) and LPS/ATP. LPS is added before or after SR9009 treatment for 3?h, followed by ATP addition for 30?min (added last).

    SR9009 purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2018;46(1):303-313.  [Abstract]

    Rev-erbα expression in relation to MMP-9 protein expression is induced by Ang II in THP-1 macrophages. MMP- 9 protein expression is analyzed by western blotting.

    • 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

    SR9009 is a REV-ERBα/β agonist with IC50s of 670 nM and 800 nM for REV-ERBα and REV-ERBβ, respectively.

    IC50 & Target

    IC50: 670 nM (Rev-ErbBα), 800 nM (Rev-ErbBβ)[1]
    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    HEK293 EC50
    0.7 μM
    Compound: 12e
    Agonist activity at Rev-Erbalpha expressed in HEK293 cells coexpressing BamII promoter assessed as repression of transcription after 24 hrs by dual-Glo luciferase assay
    Agonist activity at Rev-Erbalpha expressed in HEK293 cells coexpressing BamII promoter assessed as repression of transcription after 24 hrs by dual-Glo luciferase assay
    		[PMID: 22633688]
    HEK293 IC50
    670 nM
    Compound: 12e
    Agonist activity at Rev-Erbalpha expressed in HEK293 cells coexpressing Gal4 ligand binding domain assessed as inhibition of transcription after 24 hrs by dual-Glo luciferase assay
    Agonist activity at Rev-Erbalpha expressed in HEK293 cells coexpressing Gal4 ligand binding domain assessed as inhibition of transcription after 24 hrs by dual-Glo luciferase assay
    		[PMID: 22633688]
    體外研究
    (In Vitro)

    SR9009 以劑量依賴性方式增加在表達(dá)嵌合 Gal4 DNA 結(jié)合域 (DBD)-REV-ERB 配體結(jié)合域 (LBD) α 或 β 和 Gal4 響應(yīng)性熒光素酶報(bào)告基因 (SR9009：REV-ERBα IC50=670 nM，REV-ERBβ IC50=800 nM)。SR9009 在使用全長(zhǎng) REV-ERBα 以及由 Bmal1 啟動(dòng)子驅(qū)動(dòng)的熒光素酶報(bào)告基因的共轉(zhuǎn)染試驗(yàn)中有效地抑制轉(zhuǎn)錄 (IC50=710 nM)。SR9009 以 REV-ERBα/β 依賴性方式抑制 HepG2 細(xì)胞中 BMAL1 mRNA 的表達(dá)。使用圓二色分析 (Kd=800 nM) 也證實(shí)了 SR9009 與 REV-ERBα 的直接結(jié)合[1]。

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

    SR9009 (100 mg/kg，ip) 處理的小鼠表現(xiàn)出更嚴(yán)重的肥胖減少。在 SR9009 處理的動(dòng)物中，血漿非酯化脂肪酸 (NEFA) 和血漿葡萄糖 (19%) 也降低了 (23%)。在白色脂肪組織 (WAT) 中，SR9009 處理導(dǎo)致參與甘油三酯 (TG) 合成的編碼酶的基因表達(dá)降低，這在瘦小鼠中也觀察到了這一點(diǎn)[1]。

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

    437.94

    Formula

    C20H24ClN3O4S
    CAS 號(hào)
    性狀

    固體

    顏色

    White to off-white

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲(chǔ)存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

    DMSO 中的溶解度 : ≥ 100 mg/mL (228.34 mM; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 2.2834 mL 11.4171 mL 22.8342 mL
    5 mM 0.4567 mL 2.2834 mL 4.5668 mL
    查看完整儲(chǔ)備液配制表

    * 請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(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(dòng)物實(shí)驗(yàn)：

    請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
    ——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

    • 方案 一

      請(qǐng)依序添加每種溶劑： 5% DMSO    10% Cremophor EL    85% ddH2O

      Solubility: 20 mg/mL (45.67 mM); 懸濁液; 超聲助溶

    • 方案 二

      請(qǐng)依序添加每種溶劑： 5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: 2.5 mg/mL (5.71 mM); 懸濁液; 超聲助溶

    動(dòng)物溶解方案計(jì)算器
    請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

    給藥劑量

    mg/kg

    動(dòng)物的平均體重

    g

    每只動(dòng)物的給藥體積

    μL

    動(dòng)物數(shù)量

    只
    由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量
    請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購(gòu)。 ，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
    您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
    動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
    連續(xù)給藥周期超過(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
    請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: 99.61%

    參考文獻(xiàn)
    Cell Assay
    [1]

    HEK293 cells are grown in 96-well plates (1×106/well) and are transiently transfected using Lipofectamine. Cells are transfected with a total of 200 ng of DNA per well consisting of the pGL4 mIL-17 firefly luciferase reporter construct, the pGL4 mIL-17 + CNS-5 firefly luciferase reporter construct, or the pGL4 mIL-17 2kB RORE mutant (100 ng/well) , an actin promoter Renilla reniformis luciferase reporter (50 ng/well), and either control vector alone or the test DNA (full-length RORα or full-length RORγ at 50 ng/well). All 48 human nuclear receptors are represented in the specificity assay and SR9009 is tested at a concentration of 20 μM. The format of the assay is a cotransfection assay with Gal4 DNA binding domain-nuclear receptor fusions in HEK293 cells[1].

    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 SR9009 or 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(chǔ)備液配制表

    * 請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(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 2.2834 mL 11.4171 mL 22.8342 mL 57.0854 mL
    5 mM 0.4567 mL 2.2834 mL 4.5668 mL 11.4171 mL
    10 mM 0.2283 mL 1.1417 mL 2.2834 mL 5.7085 mL
    15 mM 0.1522 mL 0.7611 mL 1.5223 mL 3.8057 mL
    20 mM 0.1142 mL 0.5709 mL 1.1417 mL 2.8543 mL
    25 mM 0.0913 mL 0.4567 mL 0.9134 mL 2.2834 mL
    30 mM 0.0761 mL 0.3806 mL 0.7611 mL 1.9028 mL
    40 mM 0.0571 mL 0.2854 mL 0.5709 mL 1.4271 mL
    50 mM 0.0457 mL 0.2283 mL 0.4567 mL 1.1417 mL
    60 mM 0.0381 mL 0.1903 mL 0.3806 mL 0.9514 mL
    80 mM 0.0285 mL 0.1427 mL 0.2854 mL 0.7136 mL
    100 mM 0.0228 mL 0.1142 mL 0.2283 mL 0.5709 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：
    SR9009
    目錄號(hào)：
    HY-16989
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