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

Tranilast  (Synonyms: MK-341; SB 252218)

Cat. No.: HY-B0195 Purity: 99.57%
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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.

For research use only. We do not sell to patients.

Tranilast Chemical Structure

Tranilast Chemical Structure

CAS No. : 53902-12-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 73 In-stock
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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Tranilast:

Tranilast Related Antibodies

Top Publications Citing Use of Products

    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.

    View All Angiotensin Receptor Isoform Specific Products:

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    AT1 Receptor AT2 Receptor

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    DP EP FP IP TXA2/TP TXB2

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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)

    In Vitro

    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.

    Tranilast Related Antibodies

    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).
    In Vivo

    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.
    Clinical Trial
    Molecular Weight

    327.33

    Formula

    C18H17NO5
    CAS No.
    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
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    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
    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)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    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)

    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 +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    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.
    Purity & Documentation
    References

    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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    Tranilast Related Classifications

    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.

    Keywords:

    Tranilast53902-12-8MK-341 SB 252218MK341MK 341SB252218SB 252218SB-252218Angiotensin ReceptorProstaglandin ReceptorAngiogenesismicrovascularendothelialvasculargrowthfactorproliferationchemotaxistubeprostaglandinanti-atopicInhibitorinhibitorinhibit

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