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

Thapsigargin  (Synonyms: タプシガルギン; 67526-95-8)

製品番号: HY-13433 純度: 99.49%
COA 取扱説明書

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.

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Thapsigargin 構造式

Thapsigargin 構造式

CAS 番号 : 67526-95-8

容量 価格(税別) 在庫状況 数量
1 mg USD 100 在庫あり
5 mg USD 280 在庫あり
10 mg USD 450 在庫あり
25 mg USD 900 在庫あり
50 mg USD 1450 在庫あり
100 mg   お問い合わせ  
200 mg   お問い合わせ  

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カスタマーレビュー

Based on 56 publication(s) in Google Scholar

Top Publications Citing Use of Products

顧客検証

WB

    Thapsigargin purchased from MedChemExpress. 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.
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    製品説明

    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]

    体外実験

    Thapsigargin (0.001- 1 μM; for 2 and 4 days) arrests cell proliferations in MH7A human rheumatoid arthritis synovial cells in a time- and dose-dependent manner[2].
    Thapsigargin (0.001- 1 μM; for 2 and 4 days) induces cell apoptosis in MH7A cells in a time- and dose-dependent manner[2].
    Thapsigargin (0.001- 1 μM; for 2 and 4 days) impairs mTOR activity and leads to cyclin D1 expressions in MH7A cells[2].
    Thapsigargin inhibits Ca2+ entry into human neutrophil granulocytes[1].
    Thapsigargin inhibits the carbachol-evoked [Ca2+]i-transients with (IC50=0.353 nM) or without (IC50=0.448 nM) a KCl-prestimulation, but an additional small component, with a much lower sensitivity (IC50=4814 nM), is observed in the absence of a KCl-prestimulation. In contrast, the KCl-evoked [Ca2+]i-transients displayed only one component with a very low sensitivity to Thapsigargin in both absence (IC50=3343 nM) and presence (IC50=6858 nM) of a carbachol-prestimulation[3].
    Thapsigargin also phosphorylate p38 MAPK by Ca2+ influx through SOCE, leading to suppression of TNF-α-induced NF-κB phosphorylation[6].

    MedChemExpress (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
    体内実験

    Thapsigargin (Injection; 0.25 ug/g, 0.5 ug/g and 1 ug/g; 24 hours) significant increases of 2 to 5-fold in chemokine and pro-inflammatory expression. Thapsigargin is more sensitive to inducing a systemic immune response[4].

    MedChemExpress (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

    分子式

    C34H50O12

    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CCCCCCCC(O[C@@H]1[C@@H](OC(/C(C)=C\C)=O)C(C)=C2[C@@]1([H])[C@@](C)(OC(C)=O)C[C@H](OC(CCC)=O)[C@@]([C@@]3(O)C)(O)[C@@]2([H])OC3=O)=O

    Structure Classification
    Initial Source
    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件

    -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)

    溶剤 & 溶解度
    体外: 

    DMSO : 50 mg/mL (76.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    10 mM 0.1537 mL 0.7683 mL 1.5367 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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

    This equation is commonly abbreviated as: C1V1 = C2V2

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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    90% Saline

      Solubility: 5 mg/mL (7.68 mM); Suspended solution; Need ultrasonic

    • Protocol 2

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

      Solubility: ≥ 2.08 mg/mL (3.20 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
    In Vivo Dissolution Calculator
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    Please enter your animal formula composition:
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).

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

    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: 99.95%

    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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 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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    • Molarity Calculator

    • Dilution Calculator

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    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2
    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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    製品名:
    Thapsigargin
    製品番号:
    HY-13433
    数量:
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