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  3. TR-14035

TR-14035 

Cat. No.: HY-15770 Purity: 95.14%
Handling Instructions

TR-14035 is a 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 disease.

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
10 mM * 1 mL in DMSO USD 330 In-stock
Estimated Time of Arrival: December 31
5 mg USD 300 In-stock
Estimated Time of Arrival: December 31
10 mg USD 456 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1080 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1680 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products

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

    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

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    Description

    TR-14035 is a 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 disease[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 1μM, with an approximate IC50 of 0.01μM[2].

    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 plasma decreased with half-lives of 0.28 h (3 mg/kg for i.v.) and 0.39 h (10 mg/kg for i.g.), and the oral bioavailability (F) is 17%[4].

    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 i.g.
    Administration: Intravenous injection and oral gavage
    Result: T1/2 (1.88 h for i.v.; 3.42 h for i.g.), F (17%).
    Molecular Weight

    474.33

    Formula

    C₂₄H₂₁Cl₂NO₅

    CAS No.

    232271-19-1

    SMILES

    COC1=C(C2=CC=C(C[[email protected]@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 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 41 mg/mL (86.44 mM)

    *"≥" 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
    10 mM 0.2108 mL 1.0541 mL 2.1082 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

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

    *All of the co-solvents are provided by MCE.
    References
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    Keywords:

    TR-14035TR14035TR 14035Integrinallergicasthmaalpha(4)integrininflammationautoimmunediseaseInhibitorinhibitorinhibit

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