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  1. Membrane Transporter/Ion Channel Neuronal Signaling Anti-infection Apoptosis
  2. Calcium Channel SARS-CoV Apoptosis
  3. Thapsigargin

Thapsigargin  (Synonyms: 毒胡蘿卜素)

目錄號(hào): HY-13433 純度: 99.87%
COA 產(chǎn)品使用指南

Thapsigargin,內(nèi)質(zhì)網(wǎng)應(yīng)激誘導(dǎo)劑, 是一種微粒體 Ca2+-ATPase 抑制劑。Thapsigargin 能有效抑制不同細(xì)胞類(lèi)型的病毒 (HCoV-229E、MERS-CoV、COVID-19) 復(fù)制。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào),我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Thapsigargin Chemical Structure

Thapsigargin Chemical Structure

CAS No. : 67526-95-8

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Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 69 篇科研文獻(xiàn)

WB

    Thapsigargin purchased from MCE. Usage Cited in: Microbiol Spectr. 2022 Nov 15;e0328222.  [Abstract]

    Both PK-15 and 3D4/21cells are transfected with MGF110-7L-expressing plasmids with an increasing dose or empty vector and treated with Thapsigargin (TG) as positive controls. TG significant increases the levels of phosphorylated eIF2a (P-eIF2a) and ATF4 protein in the cells.
    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Thapsigargin, an endoplasmic reticulum (ER) stress inducer, is an inhibitor of microsomal Ca2+-ATPase. Thapsigargin efficiently inhibits coronavirus (HCoV-229E, MERS-CoV, SARS-CoV-2) replication in different cell types[1][2][3][4][5].

    IC50 & Target

    Ca2+-ATPase[1]

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    CCRF S-180 IC50
    30 nM
    Compound: 3; TPG
    Cytotoxicity against mouse CCRF S-180 cells incubated for 48 hrs by sulforhodamine B staining based ELISA
    Cytotoxicity against mouse CCRF S-180 cells incubated for 48 hrs by sulforhodamine B staining based ELISA
    [PMID: 33289552]
    CCRF-CEM IC50
    0.27 μM
    Compound: 6
    Cytotoxicity against human CCRF-CEM cells assessed as cell viability after 48 hrs by celltiter-blue assay
    Cytotoxicity against human CCRF-CEM cells assessed as cell viability after 48 hrs by celltiter-blue assay
    [PMID: 22582991]
    EL4 IC50
    0.1 μM
    Compound: 3; TPG
    Cytotoxicity against mouse EL4 cells incubated for 48 hrs by sulforhodamine B staining based ELISA
    Cytotoxicity against mouse EL4 cells incubated for 48 hrs by sulforhodamine B staining based ELISA
    [PMID: 33289552]
    EL4 IC50
    1.4 μM
    Compound: thapsigargin
    Cytotoxicity against mouse EL4 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay
    Cytotoxicity against mouse EL4 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay
    [PMID: 25951057]
    HL-60 IC50
    0.007 μM
    Compound: 6
    Cytotoxicity against human HL60 cells assessed as cell viability after 48 hrs by celltiter-blue assay
    Cytotoxicity against human HL60 cells assessed as cell viability after 48 hrs by celltiter-blue assay
    [PMID: 22582991]
    K562 IC50
    0.17 μM
    Compound: 6
    Cytotoxicity against human K562 cells assessed as cell viability after 48 hrs by celltiter-blue assay
    Cytotoxicity against human K562 cells assessed as cell viability after 48 hrs by celltiter-blue assay
    [PMID: 22582991]
    MCF7 IC50
    2.3 μM
    Compound: 3; TPG
    Cytotoxicity against human MCF7 cells incubated for 48 hrs by sulforhodamine B staining based ELISA
    Cytotoxicity against human MCF7 cells incubated for 48 hrs by sulforhodamine B staining based ELISA
    [PMID: 33289552]
    MCF7 IC50
    2.7 μM
    Compound: thapsigargin
    Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay
    Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay
    [PMID: 25951057]
    MCF7 GI50
    5 μM
    Compound: Thapsigargin
    Cytotoxicity against human MCF7 cells after 24 hrs by CellTiter-Glo assay
    Cytotoxicity against human MCF7 cells after 24 hrs by CellTiter-Glo assay
    [PMID: 30528127]
    PC-3 IC50
    2.4 μM
    Compound: thapsigargin
    Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay
    Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay
    [PMID: 25951057]
    體外研究
    (In Vitro)

    Thapsigargin (0.001-1 μM;持續(xù) 2 天和 4 天) 以時(shí)間和劑量依賴(lài)性方式抑制 MH7A 人類(lèi)風(fēng)濕性關(guān)節(jié)炎滑膜細(xì)胞的細(xì)胞增殖[2]
    Thapsigargin (0.001-1 μM;持續(xù) 2 天和 4 天) 以時(shí)間和劑量依賴(lài)性方式誘導(dǎo) MH7A 細(xì)胞凋亡[2]
    Thapsigargin (0.001-1 μM;持續(xù) 2 天和 4 天) 會(huì)損害 mTOR 活性并誘導(dǎo) MH7A 細(xì)胞中的細(xì)胞周期蛋白 D1 表達(dá)[2]。
    Thapsigargin 抑制Ca2+進(jìn)入人中性粒細(xì)胞[1]。
    Thapsigargin 抑制卡巴膽堿誘發(fā)的[Ca2+]i-瞬變具有 (IC50=0.353 nM) 或無(wú) (IC50=0.448 nM) KCl 預(yù)刺激,但在沒(méi)有 KCl 預(yù)刺激的情況下觀(guān)察到一個(gè)額外的小成分,靈敏度低得多 (IC50=4814 nM)。相比之下,KCl 誘發(fā)的[Ca2+]i 瞬變僅顯示一種成分,在兩種成分均不存在時(shí)對(duì) Thapsigargin 的敏感性非常低 (IC50=3343 nM) 和卡巴膽堿預(yù)刺激的存在 (IC50=6858 nM)[3]。
    Thapsigargin 還通過(guò) SOCE 流入 Ca2+ 磷酸化 p38 MAPK,從而抑制 TNF-α 誘導(dǎo)的 NF-κB 磷酸化[6]

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

    Cell Proliferation Assay[2]

    Cell Line: MH7A human rheumatoid arthritis synovial cells
    Concentration: 0.001, 0.1, and 1?μM
    Incubation Time: For 2 and 4 days
    Result: Arrested cell proliferations in a time- and dose-dependent manner.

    Apoptosis Analysis[2]

    Cell Line: MH7A human rheumatoid arthritis synovial cells
    Concentration: 0.001, 0.1, and 1?μM
    Incubation Time: For 2 and 4 days
    Result: Induces cell apoptosis in a time- and dose-dependent manner.

    Western Blot Analysis[2]

    Cell Line: MH7A human rheumatoid arthritis synovial cells
    Concentration: 0.001, 0.1, and 1?μM
    Incubation Time: For 2 and 4 days
    Result: Impairs mTOR activity and leads to cyclin D1 expressions
    體內(nèi)研究
    (In Vivo)

    Thapsigargin (注射;0.25 μg/g、0.5 μg/g 和 1 μg/g;24 小時(shí)) 趨化因子和促炎表達(dá)顯著增加 2 至 5 倍。Thapsigargin 對(duì)誘導(dǎo)全身免疫反應(yīng)更敏感[4]。

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

    Animal Model: Male Balb/c mice (20-25 g)[4]
    Dosage: 0.25 ug/g, 0.5 ug/g and 1 ug/g
    Administration: Injection; 24 hours
    Result: Increased of 2 to 5-fold in chemokine and pro-inflammatory expression.
    分子量

    650.75

    Formula

    C34H50O12

    CAS 號(hào)
    性狀

    固體

    顏色

    White to off-white

    中文名稱(chēng)

    毒胡蘿卜素;毒胡蘿卜內(nèi)酯

    結(jié)構(gòu)分類(lèi)
    初始來(lái)源
    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.

    儲(chǔ)存方式

    -20°C, sealed storage, away from moisture and light

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

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

    DMSO 中的溶解度 : 50 mg/mL (76.83 mM; 超聲助溶; 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)

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

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 1.5367 mL 7.6834 mL 15.3669 mL
    5 mM 0.3073 mL 1.5367 mL 3.0734 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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?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(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: 10% DMSO    90% Saline

      Solubility: 5 mg/mL (7.68 mM); 懸濁液; 超聲助溶

    • 方案 二

      請(qǐng)依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (3.20 mM); 澄清溶液

      此方案可獲得 ≥ 2.08 mg/mL(飽和度未知)的澄清溶液。

      1 mL 工作液為例,取 100 μL 20.8 mg/mL 的澄清 DMSO 儲(chǔ)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。
    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

    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)。

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

    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: 99.95%

    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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?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 1.5367 mL 7.6834 mL 15.3669 mL 38.4172 mL
    5 mM 0.3073 mL 1.5367 mL 3.0734 mL 7.6834 mL
    10 mM 0.1537 mL 0.7683 mL 1.5367 mL 3.8417 mL
    15 mM 0.1024 mL 0.5122 mL 1.0245 mL 2.5611 mL
    20 mM 0.0768 mL 0.3842 mL 0.7683 mL 1.9209 mL
    25 mM 0.0615 mL 0.3073 mL 0.6147 mL 1.5367 mL
    30 mM 0.0512 mL 0.2561 mL 0.5122 mL 1.2806 mL
    40 mM 0.0384 mL 0.1921 mL 0.3842 mL 0.9604 mL
    50 mM 0.0307 mL 0.1537 mL 0.3073 mL 0.7683 mL
    60 mM 0.0256 mL 0.1281 mL 0.2561 mL 0.6403 mL
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    產(chǎn)品名稱(chēng):
    Thapsigargin
    目錄號(hào):
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