1. Cytoskeleton
  2. Integrin
  3. TR-14035

TR-14035 is a orally active dual α4β74β1 integrin antagonist, with IC50 s of 7 nM and 87 nM for α4β7 and α4β1, respectively. TR-14035 can be used for the research of inflammation and autoimmune diseases.

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

TR-14035 Chemical Structure

TR-14035 Chemical Structure

CAS No. : 232271-19-1

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 230 In-stock
Solution
10 mM * 1 mL in DMSO USD 230 In-stock
Solid
1 mg USD 104 In-stock
5 mg USD 220 In-stock
10 mg USD 350 In-stock
50 mg USD 990 In-stock
100 mg USD 1500 In-stock
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500 mg   Get quote  

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Customer Review

Based on 5 publication(s) in Google Scholar

Top Publications Citing Use of Products

    TR-14035 purchased from MedChemExpress. Usage Cited in: PLoS One. 2016 Feb 3;11(2):e0148333.  [Abstract]

    Blockade of cellular adhesion of HEK 293 cells at 10 or 30 nM coated recombinant OPN forms with 1μM antagonistic integrin inhibitors. RGES (black bars) is used as a control peptide. Cilengitide (white bars) inhibits the integrins αVβ3, αVβ5, and α5β1. TR-14035 (hatched bars) inhibits the integrins α4β7 and α4β1. Depicted are the means ± SEM of 3 independent experiments. * indicate signif
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    TR-14035 is a orally active dual α4β74β1 integrin antagonist, with IC50 s of 7 nM and 87 nM for α4β7 and α4β1, respectively. TR-14035 can be used for the research of inflammation and autoimmune diseases[1][2].

    IC50 & Target[1]

    α4β7

    7 nM (IC50)

    α4β1

    87 nM (IC50)

    In Vitro

    TR14035 blocks adhesion of RPMI-8866 cells to MAdCAM-Ig by 100% at 1 μM, with an approximate IC50 of 0.01 μM[2].

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

    In Vivo

    TR-14035 (3?mg/kg; i.g.) produces a significant decrease of the airways hyper-responsiveness to 5-hydroxytryptamine (5-HT) in an experimental model of allergic asthma in Brown Norway rats[3].
    ? TR-14035 exhibits moderate oral bioavailability (rat 17.1%, dog 13.2%) and Cmax (rat 0.18, dog 0.10 μg eq./mL) following oral administration (rat 10 and dog 10 mg/kg)[4].
    ? TR-14035 exhibits terminal elimination half-lives (rat 0.28 h and, dog 0.81 h) due to high plasma clearance (3865 and 1664 mL/h/kg respectively) following intravenous administration (rat 3 mg/kg and dog 3 mg/kg)[4].

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

    Animal Model: Male Brown Norway rats (250-300 g)[3]
    Dosage: 3 mg/kg
    Administration: Oral gavage, 1 h before and 3 h after antigen challenge
    Result: Suppressed antigen-induced airway hyper-responsiveness and inflammation.
    Animal Model: Male Sprague-Dawley rats (250-320 g)[4]
    Dosage: 3 mg/ kg for i.v.; 10 mg/kg for oral (Pharmacokinetic Analysis)
    Administration: Intravenous injection and oral administration
    Result: Oral bioavailability (17.1%), Cmax (0.18 μg eq./mL), T1/2 (0.28 h).
    Animal Model: Male beagle dogs[4]
    Dosage: 3 mg/kg for i.v.; 10 mg/kg for oral (Pharmacokinetic Analysis)
    Administration: Intravenous administration and oral administration
    Result: Oral bioavailability (13.2%), Cmax ( 0.10 μg eq./mL), T1/2 (0.81 h).
    Molecular Weight

    474.33

    Formula

    C24H21Cl2NO5

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    COC1=C(C2=CC=C(C[C@@H](C(O)=O)NC(C3=C(Cl)C=CC=C3Cl)=O)C=C2)C(OC)=CC=C1

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 41 mg/mL (86.44 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1082 mL 10.5412 mL 21.0824 mL
    5 mM 0.4216 mL 2.1082 mL 4.2165 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)

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    Volume (start)

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    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 (5.27 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% Corn Oil

      Solubility: ≥ 2.5 mg/mL (5.27 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

    Dosage

    mg/kg

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    (per animal)

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    Dosing volume
    (per animal)

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    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, 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
    DMSO 1 mM 2.1082 mL 10.5412 mL 21.0824 mL 52.7059 mL
    5 mM 0.4216 mL 2.1082 mL 4.2165 mL 10.5412 mL
    10 mM 0.2108 mL 1.0541 mL 2.1082 mL 5.2706 mL
    15 mM 0.1405 mL 0.7027 mL 1.4055 mL 3.5137 mL
    20 mM 0.1054 mL 0.5271 mL 1.0541 mL 2.6353 mL
    25 mM 0.0843 mL 0.4216 mL 0.8433 mL 2.1082 mL
    30 mM 0.0703 mL 0.3514 mL 0.7027 mL 1.7569 mL
    40 mM 0.0527 mL 0.2635 mL 0.5271 mL 1.3176 mL
    50 mM 0.0422 mL 0.2108 mL 0.4216 mL 1.0541 mL
    60 mM 0.0351 mL 0.1757 mL 0.3514 mL 0.8784 mL
    80 mM 0.0264 mL 0.1318 mL 0.2635 mL 0.6588 mL
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    TR-14035 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.

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    Product Name:
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    Cat. No.:
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