1. GPCR/G Protein
  2. Angiotensin Receptor Prostaglandin Receptor
  3. Tranilast

トラニラスト  (Synonyms: Tranilast; MK-341; SB 252218)

製品番号: HY-B0195 純度: 99.95%
COA 取扱説明書 Technical Support

Tranilast (MK-341) acts as an anti-atopic agent. Tranilast suppresses production of prostaglandin D2 (PGD2, IC50= 0.1 mM). Tranilast sodium exhibits anti-inflammatory and immunomodulatory effects. Tranilast sodium antagonizes angiotensin II and inhibits its biological effects in vascular smooth muscle cells.

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号 : 53902-12-8

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 72 在庫あり
Solution
10 mM * 1 mL in DMSO USD 72 在庫あり
Solid
10 mg $66 在庫あり
50 mg $106 在庫あり
100 mg $150 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 8 publication(s) in Google Scholar

Other Forms of Tranilast:

Top Publications Citing Use of Products

    Tranilast purchased from MedChemExpress. Usage Cited in: Mol Cell. 2023 Jan 14;S1097-2765(22)01217-5.  [Abstract]

    Tranilast treatment (50 μM) on HU-induced [Ca2+]i elevation in S phase-synchronized HeLa cells treated with HU (2 mM, 4 h).

    Tranilast purchased from MedChemExpress. Usage Cited in: Mol Cell. 2023 Jan 14;S1097-2765(22)01217-5.  [Abstract]

    Tranilast treatment (50 μM) on the ER release of Ca2+ in S phase-synchronized HeLa cells treated with HU (2 mM, 4 h).

    Tranilast purchased from MedChemExpress. Usage Cited in: Mol Cell. 2023 Jan 14;S1097-2765(22)01217-5.  [Abstract]

    Effects of Tranilast treatment (50 μM) on T172-phosphorylation of AMPKα in HeLa cells treated with HU (2 mM, 4 h). γH2AX IF signal marks the cells with replication stress.

    Tranilast purchased from MedChemExpress. Usage Cited in: Mol Cell. 2023 Jan 14;S1097-2765(22)01217-5.  [Abstract]

    Effects of Tranilast treatment (50 μM) on S746-phosphorylation of Exo1-GFP in HeLa cells treated with HU (2 mM) for 4 h.

    Tranilast purchased from MedChemExpress. Usage Cited in: Mol Cell. 2023 Jan 14;S1097-2765(22)01217-5.  [Abstract]

    Effects of Tranilast on [Ca2+]i. in HeLa cells transfected with ssDNA or dsDNA fragments (2 μg/ml). Cells were imaged 6 h after transfection and Tranilast (50 μM) or DMSO was added 4 h before imaging.

    Tranilast purchased from MedChemExpress. Usage Cited in: Pharmacol Res. 2017 Nov;125(Pt B):150-160.  [Abstract]

    The IL-33 production in different treatment groups is determined in rat skin by immunohistochemistry assay.

    Angiotensin Receptor アイソフォーム固有の製品をすべて表示:

    Prostaglandin Receptor アイソフォーム固有の製品をすべて表示:

    • 生物活性

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    Tranilast (MK-341) acts as an anti-atopic agent. Tranilast suppresses production of prostaglandin D2 (PGD2, IC50= 0.1 mM). Tranilast sodium exhibits anti-inflammatory and immunomodulatory effects[1]. Tranilast sodium antagonizes angiotensin II and inhibits its biological effects in vascular smooth muscle cells[2].

    IC50 & Target

    Angiotensin II

     

    DP2

    0.1 mM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    HEK293 IC50
    126 3
    Compound: 11
    Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as inhibition of CA-induced increase in calcium influx incubated for 10 mins prior to CA addition by Fluo-4-AM dye based fluorescence assayy
    Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as inhibition of CA-induced increase in calcium influx incubated for 10 mins prior to CA addition by Fluo-4-AM dye based fluorescence assayy
    [PMID: 30878828]
    HEK293 IC50
    126 3
    Compound: 11
    Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as inhibition of CA-induced increase in calcium influx incubated for 10 mins prior to CA addition by Fluo-4-AM dye based fluorescence assayy
    Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as inhibition of CA-induced increase in calcium influx incubated for 10 mins prior to CA addition by Fluo-4-AM dye based fluorescence assayy
    [PMID: 30878828]
    RBL-2H3 IC50
    0.49 2
    Compound: Tranilast
    Inhibition of beta-hexosaminidase in anti-DNP IgE sensitized rat RBL2H3 cells after 10 mins
    Inhibition of beta-hexosaminidase in anti-DNP IgE sensitized rat RBL2H3 cells after 10 mins
    [PMID: 15387643]
    L02 IC50
    82.3 3
    Compound: 1; TR
    Antiproliferative activity against human LO2 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human LO2 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    [PMID: 36037790]
    RBL-2H3 IC50
    0.49 2
    Compound: Tranilast
    Inhibition of rat RBL2H3 cell degranulation assessed as inhibition of beta-hexosamidase release after 10 mins by microplate reader assay
    Inhibition of rat RBL2H3 cell degranulation assessed as inhibition of beta-hexosamidase release after 10 mins by microplate reader assay
    [PMID: 12398545]
    RBL-2H3 IC50
    0.49 2
    Compound: Tranilast
    Inhibition of beta-hexosaminidase in anti-DNP IgE sensitized rat RBL2H3 cells after 10 mins
    Inhibition of beta-hexosaminidase in anti-DNP IgE sensitized rat RBL2H3 cells after 10 mins
    [PMID: 15387643]
    RBL-2H3 IC50
    0.49 2
    Compound: Tranilast
    Inhibition of rat RBL2H3 cell degranulation assessed as inhibition of beta-hexosamidase release after 10 mins by microplate reader assay
    Inhibition of rat RBL2H3 cell degranulation assessed as inhibition of beta-hexosamidase release after 10 mins by microplate reader assay
    [PMID: 12398545]
    HEK293 IC50
    126 3
    Compound: 11
    Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as inhibition of CA-induced increase in calcium influx incubated for 10 mins prior to CA addition by Fluo-4-AM dye based fluorescence assayy
    Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as inhibition of CA-induced increase in calcium influx incubated for 10 mins prior to CA addition by Fluo-4-AM dye based fluorescence assayy
    [PMID: 30878828]
    L02 IC50
    82.3 3
    Compound: 1; TR
    Antiproliferative activity against human LO2 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human LO2 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    [PMID: 36037790]
    RBL-2H3 IC50
    0.49 2
    Compound: Tranilast
    Inhibition of rat RBL2H3 cell degranulation assessed as inhibition of beta-hexosamidase release after 10 mins by microplate reader assay
    Inhibition of rat RBL2H3 cell degranulation assessed as inhibition of beta-hexosamidase release after 10 mins by microplate reader assay
    [PMID: 12398545]
    RBL-2H3 IC50
    0.49 2
    Compound: Tranilast
    Inhibition of beta-hexosaminidase in anti-DNP IgE sensitized rat RBL2H3 cells after 10 mins
    Inhibition of beta-hexosaminidase in anti-DNP IgE sensitized rat RBL2H3 cells after 10 mins
    [PMID: 15387643]
    体外実験

    Tranilast exhibits significant immunomodulatory activity inhibiting Endotoxin-induced prostaglandin E2 (PGE2; IC50=~1-20 μM), thromboxane B2 (IC50=~10-50 μM), (TGF-β1; IC50=~100-200 μM), and IL-8 (IC50=~100 μM) formation. A23187-induced monocyte leukotriene C4 or PGE2 formation is inhibited by Tranilast at IC50s of 10-40 μM and 2-20 μM, respectively[3].
    Tranilast (10-200 μM) exhibits the anti-proliferative effect in a dose-dependent manner in both MCF-7 and MDA-MB-231 cell lines. Tranilast also (10-200μM) enhances the anti-tumor effects of Tamoxifen (1-20 μM) on human breast cancer cells in vitro[4].
    Tranilast (12.5, 25, 50, 100 μg/mL; 72 hours) inhibits proliferation of HDMECs[5].

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

    Cell Proliferation Assay[4]

    Cell Line: MCF-7 and MDA-MB-231 cells
    Concentration: 10, 20, 50, 100, and 200 μM
    Incubation Time: 48 hours
    Result: Anti-proliferative effect in a dose-dependent manner in both cell lines.

    Cell Viability Assay[5]

    Cell Line: Human dermal microvascular endothelial cells (HDMECs)
    Concentration: 12.5, 25, 50, 100 μg/mL
    Incubation Time: 72 hours
    Result: IC50 value was 44.3 μg/mL (136 μM).
    体内実験

    Tranilast (300 mg/kg; administered orally twice a day for 3 days) dose-dependently suppresses angiogenesis in mice[5].

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

    Animal Model: Nine-week-old male C57BL/6 mice[5]
    Dosage: 300 mg/kg
    Administration: Administered orally twice a day for 3 days
    Result: Suppressed the VEGF-induced angiogenesis in matrigel; 58% of significant suppression was observed at a dose of 300 mg/kg.
    The ED50 value and 95% confidence limits were 165 mg/kg and 162±169 mg/kg, respectively.
    分子量

    327.33

    分子式

    C18H17NO5

    CAS 番号
    Appearance

    Solid

    Color

    Light yellow to green yellow

    SMILES

    O=C(O)C1=CC=CC=C1NC(/C=C/C2=CC=C(OC)C(OC)=C2)=O

    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 : 50 mg/mL (152.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.0550 mL 15.2751 mL 30.5502 mL
    5 mM 0.6110 mL 3.0550 mL 6.1100 mL
    10 mM 0.3055 mL 1.5275 mL 3.0550 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • 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

    濃度 (開始)

    C1

    ×
    体積 (開始)

    V1

    =
    濃度 (終了)

    C2

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    体積 (終了)

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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: ≥ 2.5 mg/mL (7.64 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (7.64 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 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 (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  30% SBE-β-CD in Saline

      Solubility: 5 mg/mL (15.28 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  1.5% CMC-Na/saline water

      Solubility: 4 mg/mL (12.22 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    +
    %
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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
    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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.0550 mL 15.2751 mL 30.5502 mL 76.3755 mL
    5 mM 0.6110 mL 3.0550 mL 6.1100 mL 15.2751 mL
    10 mM 0.3055 mL 1.5275 mL 3.0550 mL 7.6376 mL
    15 mM 0.2037 mL 1.0183 mL 2.0367 mL 5.0917 mL
    20 mM 0.1528 mL 0.7638 mL 1.5275 mL 3.8188 mL
    25 mM 0.1222 mL 0.6110 mL 1.2220 mL 3.0550 mL
    30 mM 0.1018 mL 0.5092 mL 1.0183 mL 2.5459 mL
    40 mM 0.0764 mL 0.3819 mL 0.7638 mL 1.9094 mL
    50 mM 0.0611 mL 0.3055 mL 0.6110 mL 1.5275 mL
    60 mM 0.0509 mL 0.2546 mL 0.5092 mL 1.2729 mL
    80 mM 0.0382 mL 0.1909 mL 0.3819 mL 0.9547 mL
    100 mM 0.0306 mL 0.1528 mL 0.3055 mL 0.7638 mL
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    • Molarity Calculator

    • Dilution Calculator

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

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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)
    × = ×
    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:
    Tranilast
    製品番号:
    HY-B0195
    数量:
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