TR-14035
Based on 6 publication(s) in Google Scholar
TR-14035 is a orally active dual α4β7/α4β1 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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.87%
- CAS. Nr.: 232271-19-1
- Formel: C24H21Cl2NO5
- Molecular Weight:474.33
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) TR-14035
More- Cell Rep Med. 2025 Jan 16:101922. [Abstract]
- Proc Natl Acad Sci U S A. 2019 Dec 17;116(51):25860-25869. [Abstract]
- Obesity. 2015 Apr;23(4):779-85. [Abstract]
- FASEB J. 2021 Feb;35(2):e21282. [Abstract]
- Appl Biochem Biotechnol. 2026 Apr;198(4):2900-2917. [Abstract]
- PLoS One. 2016 Feb 3;11(2):e0148333. [Abstract]
Customer Validation & Images
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Cell Proliferation/Viability Assay
Biologische Aktivität
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α4β7 7 nM (IC50) |
α4β1 87 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
61 nM
Compound: 1, TR-14035
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Inhibition of Very late antigen-4 (VLA-4) expressing human leukemia cells (HL-60) aggregation with human Vascular cell adhesion molecule-1 (VCAM-1) expressing chinese hamster ovary (CHO) cells
Inhibition of Very late antigen-4 (VLA-4) expressing human leukemia cells (HL-60) aggregation with human Vascular cell adhesion molecule-1 (VCAM-1) expressing chinese hamster ovary (CHO) cells
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[PMID: 15582442] |
| Jurkat | IC50 |
0.13 nM
Compound: TR-14035
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Antagonistic activity against VLA-4 integrin of human jurkat cells using [125I]VCAM-Ig as radioligand
Antagonistic activity against VLA-4 integrin of human jurkat cells using [125I]VCAM-Ig as radioligand
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[PMID: 11591507] |
| RPMI-8866 | IC50 |
0.75 nM
Compound: TR-14035
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Inhibition of [125I]MAdCAM-Ig binding to alpha4-beta7 integrin of human RPMI-8866 cells
Inhibition of [125I]MAdCAM-Ig binding to alpha4-beta7 integrin of human RPMI-8866 cells
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[PMID: 11591507] |
| T-cell | IC50 |
99 nM
Compound: 1
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Inhibition of T cell activation assessed as CD3-VACM interaction
Inhibition of T cell activation assessed as CD3-VACM interaction
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[PMID: 17035017] |
| U-937 | IC50 |
18 nM
Compound: 1
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Inhibition of human recombinant VACM1 binding to VAL4 expressed in U937 cells by adhesion test
Inhibition of human recombinant VACM1 binding to VAL4 expressed in U937 cells by adhesion test
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[PMID: 17035017] |
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.
? 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.
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Animal Model:Male Brown Norway rats (250-300 g)[3]
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Dosage:3 mg/kg
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Administration:Oral gavage, 1 h before and 3 h after antigen challenge
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Result:Suppressed antigen-induced airway hyper-responsiveness and inflammation.
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Animal Model:Male Sprague-Dawley rats (250-320 g)[4]
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Dosage:3 mg/ kg for i.v.; 10 mg/kg for oral (Pharmacokinetic Analysis)
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Administration:Intravenous injection and oral administration
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Result:Oral bioavailability (17.1%), Cmax (0.18 μg eq./mL), T1/2 (0.28 h).
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Animal Model:Male beagle dogs[4]
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Dosage:3 mg/kg for i.v.; 10 mg/kg for oral (Pharmacokinetic Analysis)
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Administration:Intravenous administration and oral administration
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Result:Oral bioavailability (13.2%), Cmax ( 0.10 μg eq./mL), T1/2 (0.81 h).
Chemical Information
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CAS. Nr. 232271-19-1
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Appearance Solid
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Molecular Weight 474.33
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Formel C24H21Cl2NO5
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Color White to off-white
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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
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (6)
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Journal Impact Factor
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Most Recent
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Cell Rep Med
MFGE8 induces anti-PD-1 therapy resistance by promoting extracellular vesicle sorting of PD-L1. [Abstract]2025 Jan 16:101922. PMID: 39842432 -
Proc Natl Acad Sci U S A
Smad7 in intestinal CD4+ T cells determines autoimmunity in a spontaneous model of multiple sclerosis. [Abstract]2019 Dec 17;116(51):25860-25869. PMID: 31796589 -
Obesity
Immunological blockade of adipocyte inflammation caused by increased matrix metalloproteinase-cleaved osteopontin in obesity. [Abstract]2015 Apr;23(4):779-85. PMID: 25776538 -
FASEB J
Mucosal integrin α4β7 blockade fails to reduce the seeding and size of viral reservoirs in SIV-infected rhesus macaques. [Abstract]2021 Feb;35(2):e21282. PMID: 33484474 -
Appl Biochem Biotechnol
Syndecan-2 Regulates Integrin-β1 to Influence the Abnormal Subchondral Bone in Early-stage Knee Osteoarthritis. [Abstract]2026 Apr;198(4):2900-2917. PMID: 41637042 -
PLoS One
Inhibition of Cellular Adhesion by Immunological Targeting of Osteopontin Neoepitopes Generated through Matrix Metalloproteinase and Thrombin Cleavage. [Abstract]2016 Feb 3;11(2):e0148333. PMID: 26840958
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
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (210.82 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
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.
Please enter the basic information of animal experiments:
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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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Reinheit & Dokumentation
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Data Sheet (281 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Sircar I, et al. Synthesis and SAR of N-benzoyl-L-biphenylalanine derivatives: discovery of TR-14035, a dual alpha(4)beta(7)/alpha(4)beta(1) integrin antagonist. Bioorg Med Chem. 2002 Jun;10(6):2051-66. [Content Brief]
[2]. Egger LA, et al. Alpha(4)beta(7)/alpha(4)beta(1) dual integrin antagonists block alpha(4)beta(7)-dependent adhesion under shear flow. J Pharmacol Exp Ther. 2002 Jul;302(1):153-62. [Content Brief]
[3]. Julio Cortijo, et al. A small molecule, orally active, α4β1/α4β7 dual antagonist reduces leukocyte infiltration and airway hyper-responsiveness in an experimental model of allergic asthma in Brown Norway rats. Br J Pharmacol. 2006 Mar; 147(6): 661–670. [Content Brief]
[4]. M Tsuda-Tsukimoto, et al. Pharmacokinetics and metabolism of TR-14035, a novel antagonist of a4ss1/a4ss7 integrin mediated cell adhesion, in rat and dog. Xenobiotica [Content Brief]
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 |
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| 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 | |
| 100 mM | 0.0211 mL | 0.1054 mL | 0.2108 mL | 0.5271 mL |
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