1. Immunology/Inflammation
  2. STING
  3. C-176

C-176 is a selective and blood-brain barrier permeable STING inhibitor. C-176 covalently targets transmembrane cysteine residue 91 and thereby blocking activation-induced palmitoylation of STING.

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CAS 番号 : 314054-00-7

容量 価格(税別) 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 39 在庫あり
Solution
10 mM * 1 mL in DMSO USD 39 在庫あり
Solid
5 mg $36 在庫あり
10 mg $50 在庫あり
25 mg $100 在庫あり
50 mg $170 在庫あり
100 mg $250 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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カスタマーレビュー

Based on 110 publication(s) in Google Scholar

Top Publications Citing Use of Products

顧客検証

WB
IF

    C-176 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2020 May 25;17(1):165.  [Abstract]

    Western blotting indicated that the level of TBK1 phosphorylation is significantly increased after SAH. Compared with SAH + vehicle group, the phosphorylation of TBK1 is remarkably inhibited by C-176.

    C-176 purchased from MedChemExpress. Usage Cited in: Aging Cell. 2020 Aug;19(8):e13186.  [Abstract]

    The BMDMs from the young and aged mice are pretreated with C-176 (20 µM) or STING siRNA followed by stimulation with mtDNA (100 ng/ml). The C-176 treatment effectively inhibits STING activation in both young and aged BMDMs post-mtDNA stimulation, as shown by the decreased protein levels of P-STING and P-TBK1.

    C-176 purchased from MedChemExpress. Usage Cited in: Aging Cell. 2020 Aug;19(8):e13186.  [Abstract]

    The BMDMs from the young and aged mice are pretreated with C-176 (20 µM) or STING siRNA followed by stimulation with mtDNA (100 ng/ml). STING inhibition by C-176 blocks the over-activation of NLRP3 signaling in the BMDMs from the young and aged mice post-mtDNA stimulation, as shown by decreased levels of NLRP3 and Cleaved caspase-1 expression.
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    製品説明

    C-176 is a selective and blood-brain barrier permeable STING inhibitor. C-176 covalently targets transmembrane cysteine residue 91 and thereby blocking activation-induced palmitoylation of STING[1][2].

    IC50 & Target

    STING[1].

    Cellular Effect
    Cell Line Type Value Description References
    HCC1143 IC50
    9.5 μM
    Compound: 1
    Cytotoxicity against human HCC1143 cells assessed as reduction in cell viability incubated for 3 days by cell-titer-Glo reagent based assay
    Cytotoxicity against human HCC1143 cells assessed as reduction in cell viability incubated for 3 days by cell-titer-Glo reagent based assay
    [PMID: 26116180]
    HCC1806 IC50
    6.2 μM
    Compound: 1
    Cytotoxicity against human HCC1806 cells assessed as reduction in cell viability incubated for 3 days by cell-titer-Glo reagent based assay
    Cytotoxicity against human HCC1806 cells assessed as reduction in cell viability incubated for 3 days by cell-titer-Glo reagent based assay
    [PMID: 26116180]
    HCC38 IC50
    8.7 μM
    Compound: 1
    Cytotoxicity against human HCC38 cells assessed as reduction in cell viability incubated for 3 days by cell-titer-Glo reagent based assay
    Cytotoxicity against human HCC38 cells assessed as reduction in cell viability incubated for 3 days by cell-titer-Glo reagent based assay
    [PMID: 26116180]
    RAW264.7 IC50
    1.14 μM
    Compound: C-176
    Anti inflammatory activity in LPS-induced mouse RAW264.7 cells assessed as inhibition of NO production preincubated with compound for 2 hrs followed by LPS stimulation and measured after 24 hrs by griess reagent based assay
    Anti inflammatory activity in LPS-induced mouse RAW264.7 cells assessed as inhibition of NO production preincubated with compound for 2 hrs followed by LPS stimulation and measured after 24 hrs by griess reagent based assay
    [PMID: 36228412]
    体外実験

    C-176 strongly reduces STING-mediated, but not RIG-I- or TBK1-mediated, IFNβ reporter activity. Pretreatment with C-176 markedly reduce the CMA-mediated induction of serum levels of type I IFNs and IL-6[1].

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

    体内実験

    C-176 (750/375 nmol C-176 per mouse in 200 μL corn oil) significantly reduces the CMA-mediated induction of serum levels of type I IFNs and IL-6., without significant toxicity[1].
    C-176 results in a significant reduction in serum levels of type I IFNs and in a strong suppression of inflammatory parameters in the heart, with no evident signs of overt toxicity Trex1 / mice[1].
    C-176 demonstrates marked amelioration of various signs of systemic inflammation in Trex1 / mice[1].

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

    Animal Model: WT type mice.
    Dosage: 750/375 nmol C-176 per mouse in 200 μL corn oil (~1.34/0.67 mg/mL).
    Administration: Intraperitoneally, once.
    Result: Significantly reduced Serum levels of type I IFNs and IL-6.
    分子量

    358.09

    分子式

    C11H7IN2O4

    CAS 番号
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(C1=CC=C([N+]([O-])=O)O1)NC2=CC=C(I)C=C2

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 62.5 mg/mL (174.54 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Ethanol : 2.5 mg/mL (6.98 mM; ultrasonic and warming and heat to 60°C)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.7926 mL 13.9630 mL 27.9259 mL
    5 mM 0.5585 mL 2.7926 mL 5.5852 mL
    10 mM 0.2793 mL 1.3963 mL 2.7926 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

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

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

    一般には略語で表示されます: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    40% PEG300    5% Tween-80    45% Saline

      Solubility: 1.67 mg/mL (4.66 mM); Suspended solution; Need ultrasonic and warming

      This protocol yields a suspended solution of 1.67 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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.
    • Protocol 2

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

      Solubility: ≥ 0.25 mg/mL (0.70 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.25 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (2.5 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
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    (per animal)

    g

    Dosing volume
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    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
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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).
    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: 99.45%

    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    Ethanol / DMSO 1 mM 2.7926 mL 13.9630 mL 27.9259 mL 69.8149 mL
    5 mM 0.5585 mL 2.7926 mL 5.5852 mL 13.9630 mL
    DMSO 10 mM 0.2793 mL 1.3963 mL 2.7926 mL 6.9815 mL
    15 mM 0.1862 mL 0.9309 mL 1.8617 mL 4.6543 mL
    20 mM 0.1396 mL 0.6981 mL 1.3963 mL 3.4907 mL
    25 mM 0.1117 mL 0.5585 mL 1.1170 mL 2.7926 mL
    30 mM 0.0931 mL 0.4654 mL 0.9309 mL 2.3272 mL
    40 mM 0.0698 mL 0.3491 mL 0.6981 mL 1.7454 mL
    50 mM 0.0559 mL 0.2793 mL 0.5585 mL 1.3963 mL
    60 mM 0.0465 mL 0.2327 mL 0.4654 mL 1.1636 mL
    80 mM 0.0349 mL 0.1745 mL 0.3491 mL 0.8727 mL
    100 mM 0.0279 mL 0.1396 mL 0.2793 mL 0.6981 mL
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    • Molarity Calculator

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    The dilution calculator equation

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

    一般には略語で表示されます:C1V1 = C2V2

    濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
    × = ×
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    Help & FAQs
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      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

    製品名:
    C-176
    製品番号:
    HY-112906
    数量:
    MCE 日本正規代理店: