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  1. PI3K/Akt/mTOR Stem Cell/Wnt Autophagy
  2. GSK-3 Autophagy
  3. SB 216763

SB 216763是有效,選擇性和ATP競爭性的 GSK-3 抑制劑,抑制GSK-3α和GSK-3β的 IC50 為34.3 nM。

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SB 216763 Chemical Structure

SB 216763 Chemical Structure

CAS No. : 280744-09-4

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ¥715
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1 mg ¥295
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5 mg ¥650
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10 mg ¥1100
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50 mg ¥4800
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100 mg 現(xiàn)貨 詢價
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Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 33 篇科研文獻

WB
IF

    SB 216763 purchased from MCE. Usage Cited in: Biochem Pharmacol. 2018 Apr;150:280-292.  [Abstract]

    Expression of c-Myc in MKN-45 cells treated with Lanatoside C and SB216763 at indicated concentrations for 24 h.

    SB 216763 purchased from MCE. Usage Cited in: J Cell Biochem. 2018 Jul;119(7):5934-5943.  [Abstract]

    SB-216763 activates renal autophagy. Representative micrographs showing immunofluorescent staining for LC3-II for among different groups as indicated.

    SB 216763 purchased from MCE. Usage Cited in: J Cell Biochem. 2018 Jul;119(7):5934-5943.  [Abstract]

    SB-216763 activates cardiac autophagy. Images showing immunofluorescent staining for LC3-II for among different groups as indicated.

    SB 216763 purchased from MCE. Usage Cited in: J Cell Biochem. 2018 Jul;119(7):5934-5943.  [Abstract]

    SB-216763 activates cardiac autophagy. Cardiac protein expression of LC3-I, LC3-II, and p62 are assayed in cardiac tissues treated with Aldo-salt or with Aldo-salt plus SB-216763.

    SB 216763 purchased from MCE. Usage Cited in: J Cell Biochem. 2018 Jul;119(7):5934-5943.  [Abstract]

    SB-216763 activates renal autophagy. Renal protein expression of LC3-I, LC3-II and p62 are assayed in renal tissues treated with Aldo-salt or with Aldo-salt plus SB-216763. SB-216763 increased the Aldo-salt-induced autophagy.

    SB 216763 purchased from MCE. Usage Cited in: Toxicol Appl Pharmacol. 2016 Dec 15;313:195-203.  [Abstract]

    SB 216763 blocks augmentation of phosphor-glycogen synthase and depletion of inhibitory phosphorylated GSK-3β at serine 9 sites, but maintains total GSK-3β levels. Cardiac protection following SB 216763 is dependent on GSK-3β activity inhibition, not on decrease in basal GSK-3β levels. H9c2 cells are treated with 160 nM TP for 24 h after pretreatments with 2 μM SB 216763 or vehicle 2 h later. Levels of p-GS, p-GSK-3β, GSK-3β and GAPDH are measured by western blot.

    查看 GSK-3 亞型特異性產(chǎn)品:

    • 生物活性

    • 實驗參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻

    生物活性

    SB 216763 is potent, selective and ATP-competitive GSK-3 inhibitor with IC50s of 34.3 nM for both GSK-3α and GSK-3β.

    IC50 & Target[5]

    GSK-3α

    34.3 nM (IC50)

    GSK-3β

    34.3 nM (IC50)

    體外研究
    (In Vitro)

    SB-216763 (10-20 μM) induces β-catenin mediated-transcription in a dose-dependent manner in HEK293 cells. SB-216763 (10, 15 and 20 μM) can maintain mESCs with a pluripotent-like morphology in long-term culture. SB-216763 (10 μM) can maintain J1 mESCs in a pluripotent state for more than a month[2].
    SB-216763 inhibits GSK-3 with IC50 of 34 nM[3].
    SB-216763 is equally effective at inhibiting human GSK-3α and GSK-3β[5].

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

    體內(nèi)研究
    (In Vivo)

    SB216763 (20 mg/kg, i.v.) significantly improves the survival of BLM-treated mice. Mice randomized to receive BLM plus SB216763 shows a noteworthy reduction, compared with BLM-treated mice. SB216763 (20 mg/kg, i.v.) reduces the magnitude of BLM-induced alveolitis[1]. SB 216763 (0.2 mg/kg, i.v.) with either 17β-E100 or Geni100 significantly reduce infarct size when the rabbits' hearts are submitted to 30-min CAO[4].

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

    分子量

    371.22

    Formula

    C19H12Cl2N2O2

    CAS 號
    性狀

    固體

    顏色

    Orange to red

    運輸條件

    Room temperature in continental US; may vary elsewhere.

    儲存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    溶解性數(shù)據(jù)
    細胞實驗: 

    DMSO 中的溶解度 : 100 mg/mL (269.38 mM; 超聲助溶; 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)

    配制儲備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 2.6938 mL 13.4691 mL 26.9382 mL
    5 mM 0.5388 mL 2.6938 mL 5.3876 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,避免反復凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限:-80°C, 1 year; -20°C, 6 months。-80°C儲存時,請在1年內(nèi)使用, -20°C儲存時,請在6個月內(nèi)使用。

    • 摩爾計算器

    • 稀釋計算器

    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

    動物實驗:

    請根據(jù)您的 實驗動物和給藥方式 選擇適當?shù)娜芙夥桨浮?

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
    ——為保證實驗結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當保存;體內(nèi)實驗的工作液,建議您現(xiàn)用現(xiàn)配,當天使用
    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;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.73 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

      1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請依序添加每種溶劑: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (6.73 mM); 懸濁液; 超聲助溶

      此方案可獲得 2.5 mg/mL的均勻懸濁液,懸濁液可用于口服和腹腔注射。

      1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中,混合均勻。

      20% SBE-β-CD in Saline 的配制(4°C,儲存一周):2 g SBE-β-CD(磺丁基醚 β-環(huán)糊精)粉末定容于 10 mL 的生理鹽水中,完全溶解至澄清透明。
    動物溶解方案計算器
    請輸入動物實驗的基本信息:

    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

    由于實驗過程有損耗,建議您多配一只動物的量
    請輸入您的動物體內(nèi)配方組成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動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 2%。
    方案所需 助溶劑 包括:DMSO, ,均可在 MCE 網(wǎng)站選購。 ,Tween 80,均可在 MCE 網(wǎng)站選購。
    計算結(jié)果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。
    您所需的儲備液濃度超過該產(chǎn)品的實測溶解度,以下方案僅供參考,如有需要,請與 MCE 中國技術(shù)支持聯(lián)系。
    動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液,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)給藥周期超過半月以上,請謹慎選擇該方案。
    請確保第一步儲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: 99.82%

    參考文獻
    Cell Assay
    [2]

    MESCs maintained with LIF or 10 μM SB-216763 for more than a month are resuspended at 40,000 cells/mL in LIF-free mESC medium. EBs are prepared by a hanging drop procedure. Briefly, 20 μL drops containing mESCs are pipetted on the inside of a 10-cm Petri dish lid. The lids are placed onto Petri dishes containing 10 mL of HBSS and the EBs are allowed to form and grow for 4 days in the incubator. After 4 days, 15-20 EBs are transferred to a well containing LIF-free mESC medium in a 24-well plate. The medium is exchanged every two days and autonomously beating cell aggregates are observed and counted.

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

    Animal Administration
    [1]

    Mice are allocated to four groups (n=12/group) as follows: 1) intratracheal saline + vehicle (25% dimethyl sulfoxide, 25% polyethylene glycol, and 50% saline), 2) intratracheal saline + SB216763 (20 mg/kg) dissolved in vehicle, 3) intratracheal BLM (3 U/kg) + vehicle, and 4) intratracheal BLM + SB216763 (20 mg/kg) in vehicle. Another set of experiments to assess cytokine expression by reverse transcription-PCR is conducted in the mice (n=12/group) to receive 1) intratracheal saline + vehicle, 2) intratracheal BLM, and 3) intratracheal BLM + SB216763. To induce pulmonary fibrosis, BLM is intratracheally administered in mice (n=15/group) on day 0. BLM and saline-treated mice are administered with SB216763 dissolved in vehicle or vehicle alone intravenously at day 0 and then intraperitoneally twice a week until day 28. Mice are sacrificed by CO2?inhalation on days 2, 7, and 28. In the terminal deoxynucleotidyl transferase dUTP nick-end labeling (TUNEL) experiments, the cohorts of mice are as follows: saline-treated (n=6), BLM-treated (n=6), and BLM + SB216763-treated (n=6).

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

    參考文獻

    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,避免反復凍融造成的產(chǎn)品失效
    儲備液的保存方式和期限:-80°C, 1 year; -20°C, 6 months。-80°C儲存時,請在1年內(nèi)使用, -20°C儲存時,請在6個月內(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 2.6938 mL 13.4691 mL 26.9382 mL 67.3455 mL
    5 mM 0.5388 mL 2.6938 mL 5.3876 mL 13.4691 mL
    10 mM 0.2694 mL 1.3469 mL 2.6938 mL 6.7346 mL
    15 mM 0.1796 mL 0.8979 mL 1.7959 mL 4.4897 mL
    20 mM 0.1347 mL 0.6735 mL 1.3469 mL 3.3673 mL
    25 mM 0.1078 mL 0.5388 mL 1.0775 mL 2.6938 mL
    30 mM 0.0898 mL 0.4490 mL 0.8979 mL 2.2449 mL
    40 mM 0.0673 mL 0.3367 mL 0.6735 mL 1.6836 mL
    50 mM 0.0539 mL 0.2694 mL 0.5388 mL 1.3469 mL
    60 mM 0.0449 mL 0.2245 mL 0.4490 mL 1.1224 mL
    80 mM 0.0337 mL 0.1684 mL 0.3367 mL 0.8418 mL
    100 mM 0.0269 mL 0.1347 mL 0.2694 mL 0.6735 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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    Inquiry Information

    產(chǎn)品名稱:
    SB 216763
    目錄號:
    HY-12012
    需求量: